fedratinib [Ligand Id: 5716] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1287853 (Fedratinib, Sar-302503, SAR-302503, SAR302503, TG-101348, TG101348) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 26S proteasome regulatory subunit 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831205] [UniProtKB: P43686] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 3-phosphoinositide dependent protein kinase 1/3-phosphoinositide-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530] | ||||||||
| ChEMBL | Binding constant for PDPK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase AMP-activated catalytic subunit alpha 1/5`-AMP-activated protein kinase catalytic subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for AMPK-alpha1 kinase domain | B | 5.62 | pKd | 2400 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase AMP-activated catalytic subunit alpha 2/5`-AMP-activated protein kinase catalytic subunit alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2116] [GtoPdb: 1542] [UniProtKB: P54646] | ||||||||
| ChEMBL | Binding constant for AMPK-alpha2 kinase domain | B | 5.33 | pKd | 4700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase AMP-activated non-catalytic subunit gamma 1/5`-AMP-activated protein kinase subunit gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2393] [GtoPdb: 1545] [UniProtKB: P54619] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase AMP-activated non-catalytic subunit gamma 2/5`-AMP-activated protein kinase subunit gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2453] [GtoPdb: 1546] [UniProtKB: Q9UGJ0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| aarF domain containing kinase 1/AarF domain-containing protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105885] [GtoPdb: 1925] [UniProtKB: Q86TW2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.64 | pKd | 231 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Actin-related protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6090] [UniProtKB: P61160] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Actin-related protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105857] [UniProtKB: P61158] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.85 | pKd | 1419 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for TNK2 kinase domain | B | 7.19 | pKd | 64 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| activin A receptor type 1/Activin receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.88 | pKd | 1310 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ACVR1 kinase domain | B | 6.82 | pKd | 150 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| activin A receptor type 1B/Activin receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ACVR1B kinase domain | B | 5.17 | pKd | 6700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| activin A receptor type IL/Activin receptor type-1-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5311] [GtoPdb: 1784] [UniProtKB: P37023] | ||||||||
| ChEMBL | Binding constant for ACVRL1 kinase domain | B | 5.62 | pKd | 2400 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| activin A receptor type 2A/Activin receptor type-2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5616] [GtoPdb: 1791] [UniProtKB: P27037] | ||||||||
| ChEMBL | Binding constant for ACVR2A kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| activin A receptor type 2B/Activin receptor type-2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5466] [GtoPdb: 1792] [UniProtKB: Q13705] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ACVR2B kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Acyl-CoA dehydrogenase family member 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105816] [UniProtKB: Q6JQN1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Acyl-CoA dehydrogenase family member 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105707] [UniProtKB: Q709F0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenine phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105819] [UniProtKB: P07741] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenosine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3589] [GtoPdb: 1231] [UniProtKB: P55263] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenylate kinase 2, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4938] [UniProtKB: P54819] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Mitochondrial adenine nucleotide translocator 2/ADP/ATP translocase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3709670] [GtoPdb: 1063] [UniProtKB: P05141] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Mitochondrial adenine nucleotide translocator 3/ADP/ATP translocase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105854] [GtoPdb: 1064] [UniProtKB: P12236] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
| ChEMBL | Binding constant for ALK kinase domain | B | 6.19 | pKd | 650 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TEK receptor tyrosine kinase/Angiopoietin-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| ChEMBL | Binding constant for TIE2 kinase domain | B | 5.72 | pKd | 1900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ankyrin repeat and kinase domain containing 1/Ankyrin repeat and protein kinase domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5547] [GtoPdb: 1932] [UniProtKB: Q8NFD2] | ||||||||
| ChEMBL | Binding constant for ANKK1 kinase domain | B | 5.37 | pKd | 4300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| AP2 associated kinase 1/AP2-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3830] [GtoPdb: 1921] [UniProtKB: Q2M2I8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.44 | pKd | 359 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for AAK1 kinase domain | B | 7.46 | pKd | 35 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of AAK1 (unknown origin) | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| ATP-dependent 6-phosphofructokinase, platelet type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2972] [UniProtKB: Q01813] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010634] [UniProtKB: Q92499] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX3X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5553] [UniProtKB: O00571] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX42 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105782] [UniProtKB: Q86XP3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DHX30 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105814] [UniProtKB: Q7L2E3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| coenzyme Q8A/Atypical kinase COQ8A, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5550] [GtoPdb: 1927] [UniProtKB: Q8NI60] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ADCK3 kinase domain | B | 5.15 | pKd | 7000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| coenzyme Q8B/Atypical kinase COQ8B, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5753] [GtoPdb: 1928] [UniProtKB: Q96D53] | ||||||||
| ChEMBL | Binding constant for ADCK4 kinase domain | B | 6.52 | pKd | 300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for AURKA kinase domain | B | 5.36 | pKd | 4400 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.63 | pKd | 2327 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for AURKB kinase domain | B | 6.31 | pKd | 490 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| aurora kinase C/Aurora kinase C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9] | ||||||||
| ChEMBL | Binding constant for AURKC kinase domain | B | 6.46 | pKd | 350 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| neurotrophic receptor tyrosine kinase 2/BDNF/NT-3 growth factors receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] | ||||||||
| ChEMBL | Binding constant for TRKB kinase domain | B | 5.51 | pKd | 3100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| beta adrenergic receptor kinase 1/Beta-adrenergic receptor kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Bifunctional phosphoribosylaminoimidazole carboxylase/phosphoribosylaminoimidazole succinocarboxamide synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5922] [UniProtKB: P22234] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| BMP2 inducible kinase/BMP-2-inducible protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4522] [GtoPdb: 1941] [UniProtKB: Q9NSY1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.28 | pKd | 519 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for BIKE kinase domain | B | 7.49 | pKd | 32 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for BMPR1A kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238] | ||||||||
| ChEMBL | Binding constant for BMPR1B kinase domain | B | 6.39 | pKd | 410 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| bone morphogenetic protein receptor type 2/Bone morphogenetic protein receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5467] [GtoPdb: 1794] [UniProtKB: Q13873] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for BMPR2 kinase domain | B | 5.54 | pKd | 2900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| BCR activator of RhoGEF and GTPase/Breakpoint cluster region protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5146] [GtoPdb: 2755] [UniProtKB: P11274] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.76 | pKd | 1727 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
| ChEMBL | Binding affinity to recombinant human His6-TEV protease-tagged BRD4 bromodomain 1 expressed in bacteria by isothermal titration calorimetric method | B | 6.79 | pKd | 164 | nM | Kd | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| GtoPdb | - | - | 6.79 | pKd | 164 | nM | Kd | Nat Chem Biol (2014) 10: 305-12 [PMID:24584101] |
| ChEMBL | Inhibition of recombinant BRD4 BD1 (unknown origin) using H4KAc as substrate incubated for 30 mins by HTRF analysis | B | 6.04 | pIC50 | 910 | nM | IC50 | J Med Chem (2023) 66: 14150-14174 [PMID:37796543] |
| ChEMBL | Acetyl-Histone Binding Assay: Assays were performed with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were diluted in 50 mM HEPES, 150 mM NaCl, 0.1% w/v BSA, and 0.01% w/v Tween□ 20 at pH 7.5 and allowed to equilibrate to room temperature prior to addition to plates. After addition of Alpha beads to master solutions, all subsequent steps were performed in low light conditions. A 2× solution of components with final concentrations of BRD4.1 at 80 nM, Ni-coated Acceptor Bead at 25 jag/ml, and 80 nM biotinylated H4-tetra acetyl was added in 10 μL to 384-well plates (AlphaPlate-384, PerkinElmer, USA). Biotinylated peptide for BRD4.1 was synthesized in-house on a CEM Liberty 9008005 microwave peptide synthesizer: H4-tetra acetyl, biotin-PEG2-SGRGKacGGKacGLGKacGGAKacRHRK—COOH. Addition to wells was performed with either a multichannel pipet (for optimization experiments) or a Biotek EL406 liquid handler. After a 1000-rpm spin-down for 1 minute, 100 nL of the solutions of the compounds of the invention from stock plates were added by pin transfer using a Janus Workstation (PerkinElmer, USA). The streptavidin-coated donor beads (25 μg/ml final) were added as with previous solution in a 2×, 10 μL volume. Following this addition, the plates were sealed with foil to block light exposure and to prevent evaporation. The plates were spun down again at 1000 rpm for 1 minute. Next, the plates were incubated in the room with the plate reader (for temperature equilibration) for 1.5 hour prior to reading the assay. AlphaScreen□ measurements were performed on an Envision 2104 (PerkinElmer, USA) utilizing the manufacturer's protocol. | B | 6.07 | pIC50 | 850 | nM | IC50 | US-10730860-B2. Diaminopyrimidine benzenesulfone derivatives and uses thereof (2020) |
| ChEMBL | Inhibition of N-terminal 6His-tagged human BRD4 bromodomain 1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated histone H4 peptide (1 to 21 residues) containing KAc (K5/8/12/16Ac) as substrate by Alpha screen assay | B | 6.54 | pIC50 | 290 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| ChEMBL | Inhibition of BRD4 (unknown origin) | B | 6.89 | pIC50 | 130 | nM | IC50 | Eur J Med Chem (2024) 275: 116540-116540 [PMID:38852338] |
| bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21] | ||||||||
| ChEMBL | Binding affinity to human N-terminal His6-tagged BRDTexpressed in Escherichia coli BL21 (DE3) cells (21 to 137 residues) incubated for 1 hr | B | 6.79 | pKd | 164 | nM | Kd | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
| ChEMBL | Inhibition of N-terminal 6His-tagged human BRDT bromodomain 1 (21 to 137 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated histone H4 peptide (1 to 21 residues) containing KAc (K5/8/12/16Ac) as substrate by Alpha screen assay | B | 6.47 | pIC50 | 340 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| ChEMBL | Inhibition of human N-terminal His6-tagged BRDT (21 to 137 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 1 hr | B | 6.54 | pIC50 | 290 | nM | IC50 | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
| calcium/calmodulin dependent protein kinase kinase 1/Calcium/calmodulin-dependent protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5256] [GtoPdb: 1956] [UniProtKB: Q8N5S9] | ||||||||
| ChEMBL | Binding constant for CAMKK1 kinase domain | B | 5.74 | pKd | 1800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CAMKK2 kinase domain | B | 5.4 | pKd | 4000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| calcium/calmodulin dependent protein kinase I/Calcium/calmodulin-dependent protein kinase type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2493] [GtoPdb: 1952] [UniProtKB: Q14012] | ||||||||
| ChEMBL | Binding constant for CAMK1 kinase domain | B | 5.8 | pKd | 1600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| calcium/calmodulin dependent protein kinase ID/Calcium/calmodulin-dependent protein kinase type 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5073] [GtoPdb: 1953] [UniProtKB: Q8IU85] | ||||||||
| ChEMBL | Binding constant for CAMK1D kinase domain | B | 6.34 | pKd | 460 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| calcium/calmodulin dependent protein kinase IG/Calcium/calmodulin-dependent protein kinase type 1G in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5258] [GtoPdb: 1954] [UniProtKB: Q96NX5] | ||||||||
| ChEMBL | Binding constant for CAMK1G kinase domain | B | 5.49 | pKd | 3200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| calcium/calmodulin-dependent protein kinase II alpha subunit/Calcium/calmodulin-dependent protein kinase type II subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7] | ||||||||
| ChEMBL | Binding constant for CAMK2A kinase domain | B | 6.52 | pKd | 300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| calcium/calmodulin-dependent protein kinase II beta subunit/Calcium/calmodulin-dependent protein kinase type II subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554] | ||||||||
| ChEMBL | Binding constant for CAMK2B kinase domain | B | 5.17 | pKd | 6800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| calcium/calmodulin-dependent protein kinase II delta subunit/Calcium/calmodulin-dependent protein kinase type II subunit delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CAMK2D kinase domain | B | 6.23 | pKd | 590 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| calcium/calmodulin-dependent protein kinase II gamma subunit/Calcium/calmodulin-dependent protein kinase type II subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CAMK2G kinase domain | B | 6.27 | pKd | 540 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| calcium/calmodulin dependent protein kinase IV/Calcium/calmodulin-dependent protein kinase type IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CAMK4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Calcium-dependent protein kinase 1 in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908387] [UniProtKB: P62344] | ||||||||
| ChEMBL | Binding constant for PFCDPK1(P.falciparum) kinase domain | B | 5.92 | pKd | 1200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PKAC-alpha kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase, cAMP-dependent, catalytic, beta subunit/cAMP-dependent protein kinase catalytic subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2918] [GtoPdb: 1477] [UniProtKB: P22694] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PKAC-beta kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase, cAMP-dependent, catalytic, gamma subunit/cAMP-dependent protein kinase catalytic subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2743] [GtoPdb: 1478] [UniProtKB: P22612] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase X-linked/cAMP-dependent protein kinase catalytic subunit PRKX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5818] [GtoPdb: 2175] [UniProtKB: P51817] | ||||||||
| ChEMBL | Binding constant for PRKX kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase, cAMP-dependent, regulatory, type II, alpha subunit/cAMP-dependent protein kinase type II-alpha regulatory subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2221] [GtoPdb: 1474] [UniProtKB: P13861] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CSNK1A1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| casein kinase 1 alpha 1 like/Casein kinase I isoform alpha-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5520] [GtoPdb: 1996] [UniProtKB: Q8N752] | ||||||||
| ChEMBL | Binding constant for CSNK1A1L kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CSNK1D kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CSNK1E kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| casein kinase 1 gamma 1/Casein kinase I isoform gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CSNK1G1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| casein kinase 1 gamma 2/Casein kinase I isoform gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368] | ||||||||
| ChEMBL | Binding constant for CSNK1G2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CSNK1G3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400] | ||||||||
| ChEMBL | Binding constant for CSNK2A1 kinase domain | B | 6.04 | pKd | 920 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| casein kinase 2, alpha prime polypeptide subunit/Casein kinase II subunit alpha` in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.58 | pKd | 2619 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CSNK2A2 kinase domain | B | 6.92 | pKd | 120 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cell division cycle 7/Cell division cycle 7-related protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5443] [GtoPdb: 1960] [UniProtKB: O00311] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PRKG1 kinase domain | B | 5.42 | pKd | 3800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Protein kinase G (PKG) 2/cGMP-dependent protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2896] [GtoPdb: 1493] [UniProtKB: Q13237] | ||||||||
| ChEMBL | Binding constant for PRKG2 kinase domain | B | 5.8 | pKd | 1600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Choline-phosphate cytidylyltransferase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105855] [UniProtKB: P49585] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Chromodomain-helicase-DNA-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105742] [UniProtKB: Q14839] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CIT kinase domain | B | 6.85 | pKd | 140 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 11A/Cyclin-dependent kinase 11A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5416] [GtoPdb: 1963] [UniProtKB: Q9UQ88] | ||||||||
| ChEMBL | Binding constant for CDC2L2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 11B/Cyclin-dependent kinase 11B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5808] [GtoPdb: 1964] [UniProtKB: P21127] | ||||||||
| ChEMBL | Binding constant for CDC2L1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 12/Cyclin-dependent kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559692] [GtoPdb: 1965] [UniProtKB: Q9NYV4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 13/Cyclin-dependent kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795192] [GtoPdb: 1966] [UniProtKB: Q14004] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CDC2L5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 14/Cyclin-dependent kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6162] [GtoPdb: 1967] [UniProtKB: O94921] | ||||||||
| ChEMBL | Binding constant for PFTK1 kinase domain | B | 5.59 | pKd | 2600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 15/Cyclin-dependent kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5856] [GtoPdb: 1968] [UniProtKB: Q96Q40] | ||||||||
| ChEMBL | Binding constant for PFTAIRE2 kinase domain | B | 5.07 | pKd | 8600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 16/Cyclin-dependent kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4597] [GtoPdb: 1969] [UniProtKB: Q00536] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PCTK1 kinase domain | B | 5.51 | pKd | 3100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 17/Cyclin-dependent kinase 17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5790] [GtoPdb: 1970] [UniProtKB: Q00537] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PCTK2 kinase domain | B | 6.46 | pKd | 350 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 18/Cyclin-dependent kinase 18 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5316] [GtoPdb: 1971] [UniProtKB: Q07002] | ||||||||
| ChEMBL | Binding constant for PCTK3 kinase domain | B | 5.57 | pKd | 2700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 19/Cyclin-dependent kinase 19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6002] [GtoPdb: 1972] [UniProtKB: Q9BWU1] | ||||||||
| ChEMBL | Binding constant for CDK11 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CDK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Cyclin-dependent kinase 2 homolog in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908388] [UniProtKB: P61075] | ||||||||
| ChEMBL | Binding constant for PFPK5(P.falciparum) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 3/Cyclin-dependent kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4442] [GtoPdb: 1975] [UniProtKB: Q00526] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CDK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CDK4-cyclinD1 kinase domain | B | 5.3 | pKd | 5000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for CDK4-cyclinD3 kinase domain | B | 6.06 | pKd | 870 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CDK5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CDK7 kinase domain | B | 6.92 | pKd | 120 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 8/Cyclin-dependent kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5719] [GtoPdb: 1980] [UniProtKB: P49336] | ||||||||
| ChEMBL | Binding constant for CDK8 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CDK9 kinase domain | B | 5.06 | pKd | 8800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase like 1/Cyclin-dependent kinase-like 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5789] [GtoPdb: 1982] [UniProtKB: Q00532] | ||||||||
| ChEMBL | Binding constant for CDKL1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin dependent kinase like 2/Cyclin-dependent kinase-like 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5728] [GtoPdb: 1983] [UniProtKB: Q92772] | ||||||||
| ChEMBL | Binding constant for CDKL2 kinase domain | B | 5.89 | pKd | 1300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin-dependent kinase like 3/Cyclin-dependent kinase-like 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163117] [GtoPdb: 1984] [UniProtKB: Q8IVW4] | ||||||||
| ChEMBL | Binding constant for CDKL3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin-dependent kinase like 5/Cyclin-dependent kinase-like 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163112] [GtoPdb: 1986] [UniProtKB: O76039] | ||||||||
| ChEMBL | Binding constant for CDKL5 kinase domain | B | 5.14 | pKd | 7300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| cyclin G associated kinase/Cyclin-G-associated kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4355] [GtoPdb: 2027] [UniProtKB: O14976] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 7.34 | pKd | 46 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for GAK kinase domain | B | 8.96 | pKd | 1.1 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of GAK (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| Cysteine--tRNA ligase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105937] [UniProtKB: P49589] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Cytochrome c1, heme protein, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105975] [UniProtKB: P08574] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| BMX non-receptor tyrosine kinase/Cytoplasmic tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813] | ||||||||
| ChEMBL | Binding constant for BMX kinase domain | B | 5.92 | pKd | 1200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| dCTP pyrophosphatase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769292] [UniProtKB: Q9H773] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| death associated protein kinase 1/Death-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2558] [GtoPdb: 2002] [UniProtKB: P53355] | ||||||||
| ChEMBL | Binding constant for DAPK1 kinase domain | B | 7.8 | pKd | 16 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| death associated protein kinase 2/Death-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3123] [GtoPdb: 2003] [UniProtKB: Q9UIK4] | ||||||||
| ChEMBL | Binding constant for DAPK2 kinase domain | B | 7.54 | pKd | 29 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| death associated protein kinase 3/Death-associated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2468] [GtoPdb: 2004] [UniProtKB: O43293] | ||||||||
| ChEMBL | Binding constant for DAPK3 kinase domain | B | 8.92 | pKd | 1.2 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Delta(24)-sterol reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331059] [UniProtKB: Q15392] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Deoxycytidine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2447] [UniProtKB: P27707] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for DDR2 kinase domain | B | 6.02 | pKd | 950 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| DnaJ homolog subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189122] [UniProtKB: P31689] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DNA replication licensing factor MCM4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105745] [UniProtKB: P33991] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DNA topoisomerase II alpha/DNA topoisomerase 2-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DNA topoisomerase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3396] [UniProtKB: Q02880] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| dual serine/threonine and tyrosine protein kinase/Dual serine/threonine and tyrosine protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908386] [GtoPdb: 2008] [UniProtKB: Q6XUX3] | ||||||||
| ChEMBL | Binding constant for RIPK5 kinase domain | B | 5.77 | pKd | 1700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MEK1 kinase domain | B | 5.29 | pKd | 5100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MEK2 kinase domain | B | 5.51 | pKd | 3100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase 3/Dual specificity mitogen-activated protein kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2109] [GtoPdb: 2064] [UniProtKB: P46734] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MEK3 kinase domain | B | 5.46 | pKd | 3500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase 4/Dual specificity mitogen-activated protein kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2897] [GtoPdb: 2065] [UniProtKB: P45985] | ||||||||
| ChEMBL | Binding constant for MEK4 kinase domain | B | 5 | pKd | 9900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase 5/Dual specificity mitogen-activated protein kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4948] [GtoPdb: 2066] [UniProtKB: Q13163] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MEK5 kinase domain | B | 6.44 | pKd | 360 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase 6/Dual specificity mitogen-activated protein kinase kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2171] [GtoPdb: 2067] [UniProtKB: P52564] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MEK6 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase 7/Dual specificity mitogen-activated protein kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3530] [GtoPdb: 2068] [UniProtKB: O14733] | ||||||||
| ChEMBL | Binding constant for MKK7 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CLK1 kinase domain | B | 5.6 | pKd | 2500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CLK2 kinase domain | B | 5.64 | pKd | 2300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761] | ||||||||
| ChEMBL | Binding constant for CLK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CLK4 kinase domain | B | 5.7 | pKd | 2000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
| ChEMBL | Binding constant for TTK kinase domain | B | 6.35 | pKd | 450 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569] | ||||||||
| ChEMBL | Binding constant for TESK1 kinase domain | B | 5.49 | pKd | 3200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for DYRK1A kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463] | ||||||||
| ChEMBL | Binding constant for DYRK1B kinase domain | B | 5.02 | pKd | 9500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| dual specificity tyrosine phosphorylation regulated kinase 2/Dual specificity tyrosine-phosphorylation-regulated kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630] | ||||||||
| ChEMBL | Binding constant for DYRK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Dynamin-like GTPase OPA1, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105705] [UniProtKB: O60313] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| eukaryotic translation initiation factor 2 alpha kinase 4/eIF-2-alpha kinase GCN2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5358] [GtoPdb: 2018] [UniProtKB: Q9P2K8] | ||||||||
| ChEMBL | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | B | 7 | pKd | 100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TP53 regulating kinase/EKC/KEOPS complex subunit TP53RK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938223] [GtoPdb: 2248] [UniProtKB: Q96S44] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Electron transfer flavoprotein subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105744] [UniProtKB: P38117] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Elongation factor Tu, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105970] [UniProtKB: P49411] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for EPHA1 kinase domain | B | 6.14 | pKd | 730 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for EPHA2 kinase domain | B | 5.36 | pKd | 4400 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor A3/Ephrin type-A receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320] | ||||||||
| ChEMBL | Binding constant for EPHA3 kinase domain | B | 5.15 | pKd | 7100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for EPHA4 kinase domain | B | 5.4 | pKd | 4000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for EPHA5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor A6/Ephrin type-A receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4526] [GtoPdb: 1826] [UniProtKB: Q9UF33] | ||||||||
| ChEMBL | Binding constant for EPHA6 kinase domain | B | 5.41 | pKd | 3900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] | ||||||||
| ChEMBL | Binding constant for EPHA7 kinase domain | B | 5.19 | pKd | 6500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor A8/Ephrin type-A receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322] | ||||||||
| ChEMBL | Binding constant for EPHA8 kinase domain | B | 5.11 | pKd | 7700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor B1/Ephrin type-B receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762] | ||||||||
| ChEMBL | Binding constant for EPHB1 kinase domain | B | 5.77 | pKd | 1700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for EPHB2 kinase domain | B | 5.41 | pKd | 3900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for EPHB3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for EPHB4 kinase domain | B | 5.68 | pKd | 2100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| EPH receptor B6/Ephrin type-B receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for EPHB6 kinase domain | B | 6.52 | pKd | 300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for EGFR(G719C) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR(G719S) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR(S752-I759del) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR(E746-A750del) kinase domain | B | 5.21 | pKd | 6200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR(L861Q) kinase domain | B | 5.24 | pKd | 5800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR(L747-S752del, P753S) kinase domain | B | 5.25 | pKd | 5600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR(L747-T751del,Sins) kinase domain | B | 5.42 | pKd | 3800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR kinase domain | B | 5.47 | pKd | 3400 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR(L858R) kinase domain | B | 5.48 | pKd | 3300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR(L747-E749del, A750P) kinase domain | B | 5.82 | pKd | 1500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR(T790M) kinase domain | B | 6.24 | pKd | 580 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for EGFR(L858R,T790M) kinase domain | B | 6.24 | pKd | 570 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for DDR1 kinase domain | B | 5.72 | pKd | 1900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Eukaryotic peptide chain release factor GTP-binding subunit ERF3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105974] [UniProtKB: Q8IYD1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| eukaryotic translation initiation factor 2 alpha kinase 1/Eukaryotic translation initiation factor 2-alpha kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6029] [GtoPdb: 2015] [UniProtKB: Q9BQI3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for EIF2AK1 kinase domain | B | 6 | pKd | 1000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Eukaryotic translation initiation factor 5B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105852] [UniProtKB: O60841] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Exosome RNA helicase MTR4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105889] [UniProtKB: P42285] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Ferrochelatase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879831] [UniProtKB: P22830] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for FGFR1 kinase domain | B | 6.55 | pKd | 280 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| ChEMBL | Binding constant for FGFR2 kinase domain | B | 6.33 | pKd | 470 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
| ChEMBL | Binding constant for FGFR3(G697C) kinase domain | B | 6.12 | pKd | 760 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for FGFR3 kinase domain | B | 6.44 | pKd | 360 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
| ChEMBL | Binding constant for FGFR4 kinase domain | B | 5.7 | pKd | 2000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.76 | pKd | 172 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for FAK kinase domain | B | 7.38 | pKd | 42 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| General transcription and DNA repair factor IIH helicase subunit XPD in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105743] [UniProtKB: P18074] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Glycine--tRNA ligase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105815] [UniProtKB: P41250] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Glycogen phosphorylase, brain form in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3856] [UniProtKB: P11216] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Glycogen phosphorylase, liver form in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2568] [UniProtKB: P06737] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for GSK3A kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for GSK3B kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| G protein-coupled receptor kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5861] [GtoPdb: 1468] [UniProtKB: P32298] | ||||||||
| ChEMBL | Binding constant for GRK4 kinase domain | B | 6.77 | pKd | 170 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| GTP-binding nuclear protein Ran in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741190] [UniProtKB: P62826] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| GTP-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105780] [UniProtKB: Q9BZE4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Haem oxygenase 2/Heme oxygenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2546] [GtoPdb: 1442] [UniProtKB: P30519] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MET(Y1235D) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for MET kinase domain | B | 5.07 | pKd | 8500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for MET(M1250T) kinase domain | B | 5.36 | pKd | 4400 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Binding constant for TRKA kinase domain | B | 6.08 | pKd | 840 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| homeodomain interacting protein kinase 1/Homeodomain-interacting protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5427] [GtoPdb: 2033] [UniProtKB: Q86Z02] | ||||||||
| ChEMBL | Binding constant for HIPK1 kinase domain | B | 6.07 | pKd | 860 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| homeodomain interacting protein kinase 2/Homeodomain-interacting protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4576] [GtoPdb: 2034] [UniProtKB: Q9H2X6] | ||||||||
| ChEMBL | Binding constant for HIPK2 kinase domain | B | 6 | pKd | 1000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| homeodomain interacting protein kinase 3/Homeodomain-interacting protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4577] [GtoPdb: 2035] [UniProtKB: Q9H422] | ||||||||
| ChEMBL | Binding constant for HIPK3 kinase domain | B | 5.89 | pKd | 1300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| homeodomain interacting protein kinase 4/Homeodomain-interacting protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075167] [GtoPdb: 2036] [UniProtKB: Q8NE63] | ||||||||
| ChEMBL | Binding constant for HIPK4 kinase domain | B | 6.66 | pKd | 220 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| hormonally up-regulated Neu-associated kinase/Hormonally up-regulated neu tumor-associated kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795165] [GtoPdb: 2037] [UniProtKB: P57058] | ||||||||
| ChEMBL | Binding constant for HUNK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa-B kinase subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111] | ||||||||
| ChEMBL | Binding constant for IKK-alpha kinase domain | B | 6.08 | pKd | 830 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] | ||||||||
| ChEMBL | Binding constant for IKK-beta kinase domain | B | 6.44 | pKd | 360 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa-B kinase subunit epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.65 | pKd | 2264 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for IKK-epsilon kinase domain | B | 6.44 | pKd | 360 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| inosine monophosphate dehydrogenase 2/Inosine-5`-monophosphate dehydrogenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2002] [GtoPdb: 2625] [UniProtKB: P12268] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for IGF1R kinase domain | B | 5.66 | pKd | 2200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for INSR kinase domain | B | 6.07 | pKd | 850 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Insulin receptor-related receptor/Insulin receptor-related protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5483] [GtoPdb: 1802] [UniProtKB: P14616] | ||||||||
| ChEMBL | Binding constant for INSRR kinase domain | B | 5.8 | pKd | 1600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| integrin linked kinase/Integrin-linked protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5247] [GtoPdb: 2041] [UniProtKB: Q13418] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525] | ||||||||
| ChEMBL | Binding constant for PRKR kinase domain | B | 5.96 | pKd | 1100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for IRAK1 kinase domain | B | 6.66 | pKd | 220 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| interleukin 1 receptor associated kinase 3/Interleukin-1 receptor-associated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5081] [GtoPdb: 2044] [UniProtKB: Q9Y616] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.85 | pKd | 1415 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for IRAK3 kinase domain | B | 6.92 | pKd | 120 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for IRAK4 kinase domain | B | 5.92 | pKd | 1200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Isoleucine--tRNA ligase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105821] [UniProtKB: Q9NSE4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007] | ||||||||
| ChEMBL | Binding constant for LRRK2(G2019S) kinase domain | B | 6 | pKd | 1000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for LRRK2 kinase domain | B | 6.06 | pKd | 870 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376] | ||||||||
| ChEMBL | Binding constant for LTK kinase domain | B | 5.2 | pKd | 6300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for LIMK1 kinase domain | B | 6.03 | pKd | 940 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| LIM domain kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5932] [GtoPdb: 2055] [UniProtKB: P53671] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for LIMK2 kinase domain | B | 5.1 | pKd | 7900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| ChEMBL | Binding constant for CSF1R kinase domain | B | 6.21 | pKd | 620 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MST1R kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MAPKAPK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MAPKAPK5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5] | ||||||||
| ChEMBL | Binding constant for MKNK1 kinase domain | B | 5.14 | pKd | 7300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] | ||||||||
| ChEMBL | Binding constant for MKNK2 kinase domain | B | 6.42 | pKd | 380 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MARK3 kinase domain | B | 6.52 | pKd | 300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MARK4 kinase domain | B | 6.01 | pKd | 970 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Binding constant for KIT(V559D,V654A) kinase domain | B | 5.46 | pKd | 3500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for KIT(V559D,T670I) kinase domain | B | 5.82 | pKd | 1500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for KIT(D816H) kinase domain | B | 6.8 | pKd | 160 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for KIT(D816V) kinase domain | B | 6.8 | pKd | 160 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for KIT kinase domain | B | 6.89 | pKd | 130 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for KIT(L576P) kinase domain | B | 6.92 | pKd | 120 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for KIT(V559D) kinase domain | B | 7.24 | pKd | 58 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for KIT(A829P) kinase domain | B | 7.34 | pKd | 46 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MELK kinase domain | B | 5.59 | pKd | 2600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| megakaryocyte-associated tyrosine kinase/Megakaryocyte-associated tyrosine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4175] [GtoPdb: 2101] [UniProtKB: P42679] | ||||||||
| ChEMBL | Binding constant for CTK kinase domain | B | 5.77 | pKd | 1700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Membrane-associated progesterone receptor component 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105706] [UniProtKB: O00264] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, membrane associated tyrosine/threonine 1/Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PKMYT1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Microtubule associated serine/threonine kinase 1/Microtubule-associated serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163128] [GtoPdb: 1510] [UniProtKB: Q9Y2H9] | ||||||||
| ChEMBL | Binding constant for MAST1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| misshapen like kinase 1/Misshapen-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8] | ||||||||
| ChEMBL | Binding constant for MINK kinase domain | B | 5.05 | pKd | 8900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ERK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 10/Mitogen-activated protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for JNK3 kinase domain | B | 6.7 | pKd | 200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 11/Mitogen-activated protein kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for p38-beta kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 12/Mitogen-activated protein kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778] | ||||||||
| ChEMBL | Binding constant for p38-gamma kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 13/Mitogen-activated protein kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2939] [GtoPdb: 1502] [UniProtKB: O15264] | ||||||||
| ChEMBL | Binding constant for p38-delta kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for p38-alpha kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ERK8 kinase domain | B | 6.29 | pKd | 510 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ERK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 4/Mitogen-activated protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5759] [GtoPdb: 2091] [UniProtKB: P31152] | ||||||||
| ChEMBL | Binding constant for ERK4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 6/Mitogen-activated protein kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5121] [GtoPdb: 2092] [UniProtKB: Q16659] | ||||||||
| ChEMBL | Binding constant for ERK3 kinase domain | B | 5.92 | pKd | 1200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.88 | pKd | 1311 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ERK5 kinase domain | B | 7.18 | pKd | 66 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 8/Mitogen-activated protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.65 | pKd | 2223 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for JNK1 kinase domain | B | 6.59 | pKd | 260 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase 9/Mitogen-activated protein kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.8 | pKd | 1571 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for JNK2 kinase domain | B | 6.62 | pKd | 240 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MAP3K1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 10/Mitogen-activated protein kinase kinase kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2873] [GtoPdb: 2070] [UniProtKB: Q02779] | ||||||||
| ChEMBL | Binding constant for MLK2 kinase domain | B | 5.16 | pKd | 6900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MLK3 kinase domain | B | 5.51 | pKd | 3100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 12/Mitogen-activated protein kinase kinase kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908389] [GtoPdb: 2072] [UniProtKB: Q12852] | ||||||||
| ChEMBL | Binding constant for DLK kinase domain | B | 5.2 | pKd | 6300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 13/Mitogen-activated protein kinase kinase kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163124] [GtoPdb: 2073] [UniProtKB: O43283] | ||||||||
| ChEMBL | Binding constant for LZK kinase domain | B | 6.23 | pKd | 590 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 15/Mitogen-activated protein kinase kinase kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163127] [GtoPdb: 2075] [UniProtKB: Q6ZN16] | ||||||||
| ChEMBL | Binding constant for MAP3K15 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 19/Mitogen-activated protein kinase kinase kinase 19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6191] [GtoPdb: 2076] [UniProtKB: Q56UN5] | ||||||||
| ChEMBL | Binding constant for YSK4 kinase domain | B | 7.72 | pKd | 19 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5914] [GtoPdb: 2077] [UniProtKB: Q9Y2U5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MAP3K2 kinase domain | B | 6.24 | pKd | 580 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mitogen-activated protein kinase kinase kinase 20 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ZAK kinase domain | B | 6.19 | pKd | 650 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5970] [GtoPdb: 2078] [UniProtKB: Q99759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MAP3K3 kinase domain | B | 5.89 | pKd | 1300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4853] [GtoPdb: 2079] [UniProtKB: Q9Y6R4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MAP3K4 kinase domain | B | 5.39 | pKd | 4100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ASK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 6/Mitogen-activated protein kinase kinase kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163123] [GtoPdb: 2081] [UniProtKB: O95382] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ASK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318] | ||||||||
| ChEMBL | Binding constant for TAK1 kinase domain | B | 5.51 | pKd | 3100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192] | ||||||||
| ChEMBL | Binding constant for MLK1 kinase domain | B | 5.49 | pKd | 3200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5749] [GtoPdb: 2085] [UniProtKB: Q92918] | ||||||||
| ChEMBL | Binding constant for HPK1 kinase domain | B | 5.89 | pKd | 1300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MAP4K2 kinase domain | B | 5.68 | pKd | 2100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MAP4K3 kinase domain | B | 5.74 | pKd | 1800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6166] [GtoPdb: 2088] [UniProtKB: O95819] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MAP4K4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mitogen-activated protein kinase kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4852] [GtoPdb: 2089] [UniProtKB: Q9Y4K4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MAP4K5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| muscle associated receptor tyrosine kinase/Muscle, skeletal receptor tyrosine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5684] [GtoPdb: 1847] [UniProtKB: O15146] | ||||||||
| ChEMBL | Binding constant for MUSK kinase domain | B | 6.1 | pKd | 800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Myosin-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105746] [UniProtKB: P35580] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Myosin-14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105888] [UniProtKB: Q7Z406] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| myosin IIIA/Myosin-IIIa in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5546] [GtoPdb: 2112] [UniProtKB: Q8NEV4] | ||||||||
| ChEMBL | Binding constant for MYO3A kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| myosin IIIB/Myosin-IIIb in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5654] [GtoPdb: 2113] [UniProtKB: Q8WXR4] | ||||||||
| ChEMBL | Binding constant for MYO3B kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| myosin light chain kinase 3/Myosin light chain kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4627] [GtoPdb: 2110] [UniProtKB: Q32MK0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MLCK kinase domain | B | 5.01 | pKd | 9700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| myosin light chain kinase 2/Myosin light chain kinase 2, skeletal/cardiac muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2777] [GtoPdb: 1553] [UniProtKB: Q9H1R3] | ||||||||
| ChEMBL | Binding constant for MYLK2 kinase domain | B | 5.52 | pKd | 3000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| myosin light chain kinase family member 4/Myosin light chain kinase family member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5426] [GtoPdb: 2111] [UniProtKB: Q86YV6] | ||||||||
| ChEMBL | Binding constant for MYLK4 kinase domain | B | 6.89 | pKd | 130 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MYLK kinase domain | B | 6.28 | pKd | 520 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| DM1 protein kinase/Myotonin-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5320] [GtoPdb: 1505] [UniProtKB: Q09013] | ||||||||
| ChEMBL | Binding constant for DMPK kinase domain | B | 6 | pKd | 1000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105781] [UniProtKB: Q9P0J0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for TNK1 kinase domain | B | 6.44 | pKd | 360 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | B | 6.35 | pKd | 450 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding affinity to recombinant human TYK2 kinase domain by fluorescence polarization assay | B | 6.66 | pKd | 217 | nM | Kd | J Med Chem (2024) 67: 10012-10024 [PMID:38843875] |
| ChEMBL | Binding constant for TYK2(JH1domain-catalytic) kinase domain | B | 7.68 | pKd | 21 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of human TYK2 | B | 6.39 | pKi | 405 | nM | Ki | J Med Chem (2018) 61: 9030-9058 [PMID:29870256] |
| ChEMBL | Inhibition of recombinant human TYK2 assessed as inhibition of substrate phosphorylation measured every 5 mins for 30 mins by LANCE Ultra kinase assay | B | 5.43 | pIC50 | 3714 | nM | IC50 | J Med Chem (2024) 67: 10012-10024 [PMID:38843875] |
| ChEMBL | Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s). | B | 6.51 | pIC50 | 310 | nM | IC50 | US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018) |
| ChEMBL | Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. | B | 6.51 | pIC50 | 310 | nM | IC50 | US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020) |
| ChEMBL | Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. | B | 6.51 | pIC50 | 310 | nM | IC50 | US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021) |
| ChEMBL | Inhibition of TYK2 (unknown origin) | B | 6.7 | pIC50 | 200.8 | nM | IC50 | J Med Chem (2023) 66: 5753-5773 [PMID:37057760] |
| GtoPdb | - | - | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7454-7 [PMID:21106455] |
| ChEMBL | Inhibition of human recombinant TYK2 by TR-FRET assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7454-7457 [PMID:21106455] |
| ChEMBL | Inhibition of TYK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescent assay | B | 6.92 | pIC50 | 121 | nM | IC50 | J Med Chem (2023) 66: 14150-14174 [PMID:37796543] |
| neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288] | ||||||||
| ChEMBL | Binding constant for TRKC kinase domain | B | 5.07 | pKd | 8600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285] | ||||||||
| ChEMBL | Binding constant for ARK5 kinase domain | B | 7.47 | pKd | 34 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| NUAK family, SNF1-like kinase, 2/NUAK family SNF1-like kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5698] [GtoPdb: 2130] [UniProtKB: Q9H093] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for SNARK kinase domain | B | 7.31 | pKd | 49 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Obg-like ATPase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105704] [UniProtKB: Q9NTK5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin dependent serine protein kinase/Peripheral plasma membrane protein CASK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908381] [GtoPdb: 1959] [UniProtKB: O14936] | ||||||||
| ChEMBL | Binding constant for CASK kinase domain | B | 5.55 | pKd | 2800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Peroxisomal acyl-coenzyme A oxidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105748] [UniProtKB: Q15067] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Peroxisomal acyl-coenzyme A oxidase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105817] [UniProtKB: O15254] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Phenylalanine--tRNA ligase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105969] [UniProtKB: Q9NSD9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Phosphatidylethanolamine-binding protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105856] [UniProtKB: P30086] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma/Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163120] [GtoPdb: 2288] [UniProtKB: O75747] | ||||||||
| ChEMBL | Binding constant for PIK3C2G kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| ChEMBL | Binding constant for PIK3CA kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for PIK3CA(C420R) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for PIK3CA(E542K) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for PIK3CA(E545A) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for PIK3CA(E545K) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for PIK3CA(Q546K) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for PIK3CA(H1047Y) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for PIK3CA(I800L) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for PIK3CA(M1043I) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for PIK3CA(H1047L) kinase domain | B | 5.41 | pKd | 3900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
| ChEMBL | Binding constant for PIK3CB kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] | ||||||||
| ChEMBL | Binding constant for PIK3CD kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
| ChEMBL | Binding constant for PIK3CG kinase domain | B | 5.12 | pKd | 7500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphatidylinositol 4-kinase beta/Phosphatidylinositol 4-kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8] | ||||||||
| ChEMBL | Binding constant for PIK4CB kinase domain | B | 5.77 | pKd | 1700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750] | ||||||||
| ChEMBL | Binding constant for PIK3C2B kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphatidylinositol-4-phosphate 5-kinase type 1 alpha/Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5969] [GtoPdb: 2164] [UniProtKB: Q99755] | ||||||||
| ChEMBL | Binding constant for PIP5K1A kinase domain | B | 7.18 | pKd | 66 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphatidylinositol-4-phosphate 5-kinase type 1 gamma/Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908383] [GtoPdb: 2165] [UniProtKB: O60331] | ||||||||
| ChEMBL | Binding constant for PIP5K1C kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphatidylinositol-5-phosphate 4-kinase type 2 alpha/Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795194] [GtoPdb: 2858] [UniProtKB: P48426] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| phosphatidylinositol-5-phosphate 4-kinase type 2 beta/Phosphatidylinositol 5-phosphate 4-kinase type-2 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5667] [GtoPdb: 2162] [UniProtKB: P78356] | ||||||||
| ChEMBL | Binding constant for PIP5K2B kinase domain | B | 6.8 | pKd | 160 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphatidylinositol-5-phosphate 4-kinase type 2 gamma/Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770034] [GtoPdb: 2163] [UniProtKB: Q8TBX8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PIP5K2C kinase domain | B | 5.39 | pKd | 4100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PHKG2 kinase domain | B | 5.8 | pKd | 1600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| phosphorylase kinase catalytic subunit gamma 1/Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4004] [GtoPdb: 2145] [UniProtKB: Q16816] | ||||||||
| ChEMBL | Binding constant for PHKG1 kinase domain | B | 6.48 | pKd | 330 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] | ||||||||
| ChEMBL | Binding constant for PDGFRA kinase domain | B | 5.57 | pKd | 2700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| ChEMBL | Binding constant for PDGFRB kinase domain | B | 7.35 | pKd | 45 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Probable ATP-dependent RNA helicase DDX6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105783] [UniProtKB: P26196] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Protein delta homolog 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5671] [UniProtKB: P80370] | ||||||||
| ChEMBL | Binding affinity to DLK (unknown origin) assessed as dissociation constant | B | 5.2 | pKd | 6300 | nM | Kd | Eur J Med Chem (2023) 255: 115404-115404 [PMID:37098296] |
| protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C beta/Protein kinase C beta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C delta/Protein kinase C delta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PRKCD kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase C epsilon/Protein kinase C epsilon type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156] | ||||||||
| ChEMBL | Binding constant for PRKCE kinase domain | B | 5.09 | pKd | 8100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase C eta/Protein kinase C eta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723] | ||||||||
| ChEMBL | Binding constant for PRKCH kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase C iota/Protein kinase C iota type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PRKCI kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase C theta/Protein kinase C theta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PRKCQ kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PYK2 kinase domain | B | 6.66 | pKd | 220 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for BRK kinase domain | B | 5.92 | pKd | 1200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.79 | pKd | 1638 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for RET(M918T) kinase domain | B | 6.82 | pKd | 150 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for RET kinase domain | B | 6.89 | pKd | 130 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for RET(V804M) kinase domain | B | 7.09 | pKd | 81 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for RET(V804L) kinase domain | B | 7.15 | pKd | 71 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of RET in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.18 | pIC50 | 6607.9 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of RET in human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.75 | pIC50 | 1779.3 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of RET in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.78 | pIC50 | 1660.6 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of RET in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.83 | pIC50 | 1469.5 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of RET in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.95 | pIC50 | 1123 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of RET in Melphalan Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6.42 | pIC50 | 381.2 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of RET (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescent assay | B | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (2023) 66: 14150-14174 [PMID:37796543] |
| ChEMBL | Inhibition of RET (unknown origin) | B | 7.32 | pIC50 | 48 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| ChEMBL | Inhibition of RET (unknown origin) | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
| ChEMBL | Inhibition of RET (unknown origin) | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
| c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922] | ||||||||
| ChEMBL | Binding constant for ROS1 kinase domain | B | 6.22 | pKd | 600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for SRC kinase domain | B | 7.12 | pKd | 75 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Putative heat shock protein HSP 90-beta 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105858] [UniProtKB: Q58FF8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Pyridoxal kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075181] [UniProtKB: O00764] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Rab-like protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105853] [UniProtKB: Q5HYI8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for AKT1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| AKT serine/threonine kinase 2/RAC-beta serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for AKT2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| AKT serine/threonine kinase 3/RAC-gamma serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for AKT3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Raf-1 proto-oncogene, serine/threonine kinase/RAF proto-oncogene serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] | ||||||||
| ChEMBL | Binding constant for RAF1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Ras-related protein Rab-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105971] [UniProtKB: P61026] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| RAB27A, member RAS oncogene family/Ras-related protein Rab-27A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105702] [GtoPdb: 2916] [UniProtKB: P51159] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Ras-related protein Rab-6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105703] [UniProtKB: P20340] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546] | ||||||||
| ChEMBL | Binding constant for RIPK1 kinase domain | B | 5.28 | pKd | 5300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| receptor interacting serine/threonine kinase 2/Receptor-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for RIPK2 kinase domain | B | 5.21 | pKd | 6100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| receptor interacting serine/threonine kinase 4/Receptor-interacting serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6083] [GtoPdb: 2192] [UniProtKB: P57078] | ||||||||
| ChEMBL | Binding constant for RIPK4 kinase domain | B | 5.01 | pKd | 9800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.17 | pKd | 670 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for FLT3(R834Q) kinase domain | B | 7.54 | pKd | 29 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for FLT3(N841I) kinase domain | B | 7.7 | pKd | 20 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for FLT3(ITD) kinase domain | B | 7.8 | pKd | 16 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for FLT3(K663Q) kinase domain | B | 7.89 | pKd | 13 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for FLT3 kinase domain | B | 7.89 | pKd | 13 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for FLT3(D835Y) kinase domain | B | 8.19 | pKd | 6.4 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for FLT3(D835H) kinase domain | B | 8.31 | pKd | 4.9 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of FLT3 in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.18 | pIC50 | 6607.9 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of FLT3 in human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.75 | pIC50 | 1779.3 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of FLT3 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.78 | pIC50 | 1660.6 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of FLT3 in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.83 | pIC50 | 1469.5 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of FLT3 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.95 | pIC50 | 1123 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of FLT3 in Melphalan Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6.42 | pIC50 | 381.2 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of FLT3 (unknown origin) | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
| ChEMBL | Inhibition of FLT3 (unknown origin) | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
| ChEMBL | Inhibition of FLT3 (unknown origin) | B | 7.82 | pIC50 | 15 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| ChEMBL | Inhibition of FLT3 (unknown origin) | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986] |
| ChEMBL | Inhibition of FLT3 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescent assay | B | 7.98 | pIC50 | 10.4 | nM | IC50 | J Med Chem (2023) 66: 14150-14174 [PMID:37796543] |
| erb-b2 receptor tyrosine kinase 2/Receptor tyrosine-protein kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Binding constant for ERBB2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| erb-b2 receptor tyrosine kinase 3/Receptor tyrosine-protein kinase erbB-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5838] [GtoPdb: 1798] [UniProtKB: P21860] | ||||||||
| ChEMBL | Binding constant for ERBB3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| erb-b2 receptor tyrosine kinase 4/Receptor tyrosine-protein kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303] | ||||||||
| ChEMBL | Binding constant for ERBB4 kinase domain | B | 5.7 | pKd | 2000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ROCK1 kinase domain | B | 5.68 | pKd | 2100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ROCK2 kinase domain | B | 5.66 | pKd | 2200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| G protein-coupled receptor kinase 1/Rhodopsin kinase GRK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5607] [GtoPdb: 1465] [UniProtKB: Q15835] | ||||||||
| ChEMBL | Binding constant for GRK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| G protein-coupled receptor kinase 7/Rhodopsin kinase GRK7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075133] [GtoPdb: 1471] [UniProtKB: Q8WTQ7] | ||||||||
| ChEMBL | Binding constant for GRK7 kinase domain | B | 5.59 | pKd | 2600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain | B | 5.92 | pKd | 1200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain | B | 6.38 | pKd | 420 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349] | ||||||||
| ChEMBL | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | B | 5.11 | pKd | 7700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain | B | 5.64 | pKd | 2300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain | B | 5.09 | pKd | 8100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain | B | 6.85 | pKd | 140 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain | B | 5.36 | pKd | 4400 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain | B | 5.66 | pKd | 2200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for RSK4(Kin.Dom.1-N-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | B | 6.44 | pKd | 360 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
| ChEMBL | Binding constant for S6K1 kinase domain | B | 5.7 | pKd | 2000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Ribosyldihydronicotinamide dehydrogenase [quinone] in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.37 | pKd | 4314 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| RNA cytidine acetyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105935] [UniProtKB: Q9H0A0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| S-adenosylmethionine synthase isoform type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3313835] [UniProtKB: P31153] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Septin-9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105891] [UniProtKB: Q9UHD8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for LOK kinase domain | B | 5.54 | pKd | 2900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 16/Serine/threonine-protein kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3938] [GtoPdb: 2213] [UniProtKB: O75716] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.25 | pKd | 566 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for STK16 kinase domain | B | 8.18 | pKd | 6.6 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 17a/Serine/threonine-protein kinase 17A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4525] [GtoPdb: 2214] [UniProtKB: Q9UEE5] | ||||||||
| ChEMBL | Binding constant for DRAK1 kinase domain | B | 6.21 | pKd | 610 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 17b/Serine/threonine-protein kinase 17B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3980] [GtoPdb: 2215] [UniProtKB: O94768] | ||||||||
| ChEMBL | Binding constant for DRAK2 kinase domain | B | 7.35 | pKd | 45 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MST3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 25/Serine/threonine-protein kinase 25 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5552] [GtoPdb: 2218] [UniProtKB: O00506] | ||||||||
| ChEMBL | Binding constant for YSK1 kinase domain | B | 5.14 | pKd | 7200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MST4 kinase domain | B | 5.12 | pKd | 7500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MST2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 32A/Serine/threonine-protein kinase 32A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6150] [GtoPdb: 1537] [UniProtKB: Q8WU08] | ||||||||
| ChEMBL | Binding constant for YANK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 32B/Serine/threonine-protein kinase 32B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5912] [GtoPdb: 1538] [UniProtKB: Q9NY57] | ||||||||
| ChEMBL | Binding constant for YANK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 32C/Serine/threonine-protein kinase 32C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5405] [GtoPdb: 1539] [UniProtKB: Q86UX6] | ||||||||
| ChEMBL | Binding constant for YANK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 33/Serine/threonine-protein kinase 33 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6005] [GtoPdb: 2221] [UniProtKB: Q9BYT3] | ||||||||
| ChEMBL | Binding constant for STK33 kinase domain | B | 6.66 | pKd | 220 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 35/Serine/threonine-protein kinase 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5651] [GtoPdb: 2222] [UniProtKB: Q8TDR2] | ||||||||
| ChEMBL | Binding constant for STK35 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 36/Serine/threonine-protein kinase 36 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4312] [GtoPdb: 2223] [UniProtKB: Q9NRP7] | ||||||||
| ChEMBL | Binding constant for STK36 kinase domain | B | 6.06 | pKd | 870 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Serine/threonine kinase 38/Serine/threonine-protein kinase 38 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075155] [GtoPdb: 1517] [UniProtKB: Q15208] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for NDR1 kinase domain | B | 5.24 | pKd | 5800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Serine/threonine kinase 38 like/Serine/threonine-protein kinase 38-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4851] [GtoPdb: 1518] [UniProtKB: Q9Y2H1] | ||||||||
| ChEMBL | Binding constant for NDR2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MST1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for BRAF kinase domain | B | 5.01 | pKd | 9800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for BRAF(V600E) kinase domain | B | 5.03 | pKd | 9300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| BR serine/threonine kinase 1/Serine/threonine-protein kinase BRSK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5650] [GtoPdb: 1946] [UniProtKB: Q8TDC3] | ||||||||
| ChEMBL | Binding constant for BRSK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| BR serine/threonine kinase 2/Serine/threonine-protein kinase BRSK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3] | ||||||||
| ChEMBL | Binding constant for BRSK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CHEK1 kinase domain | B | 5.42 | pKd | 3800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017] | ||||||||
| ChEMBL | Binding constant for CHEK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase D1/Serine/threonine-protein kinase D1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139] | ||||||||
| ChEMBL | Binding constant for PRKD1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PRKD2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase D3/Serine/threonine-protein kinase D3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PRKD3 kinase domain | B | 5.02 | pKd | 9600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| doublecortin like kinase 1/Serine/threonine-protein kinase DCLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5683] [GtoPdb: 2005] [UniProtKB: O15075] | ||||||||
| ChEMBL | Binding constant for DCAMKL1 kinase domain | B | 6.72 | pKd | 190 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| doublecortin like kinase 2/Serine/threonine-protein kinase DCLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5519] [GtoPdb: 2006] [UniProtKB: Q8N568] | ||||||||
| ChEMBL | Binding constant for DCAMKL2 kinase domain | B | 6.06 | pKd | 870 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| doublecortin like kinase 3/Serine/threonine-protein kinase DCLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6123] [GtoPdb: 2007] [UniProtKB: Q9C098] | ||||||||
| ChEMBL | Binding constant for DCAMKL3 kinase domain | B | 7.89 | pKd | 13 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| endoplasmic reticulum to nucleus signaling 1/Serine/threonine-protein kinase/endoribonuclease IRE1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163101] [GtoPdb: 2020] [UniProtKB: O75460] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ERN1 kinase domain | B | 5.92 | pKd | 1200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| endoplasmic reticulum to nucleus signaling 2/Serine/threonine-protein kinase/endoribonuclease IRE2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105932] [GtoPdb: 2021] [UniProtKB: Q76MJ5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ciliogenesis associated kinase 1/Serine/threonine-protein kinase ICK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163126] [GtoPdb: 2038] [UniProtKB: Q9UPZ9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ICK kinase domain | B | 5.72 | pKd | 1900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for LATS1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| large tumor suppressor kinase 2/Serine/threonine-protein kinase LATS2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5907] [GtoPdb: 1516] [UniProtKB: Q9NRM7] | ||||||||
| ChEMBL | Binding constant for LATS2 kinase domain | B | 5.1 | pKd | 8000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| male germ cell associated kinase/Serine/threonine-protein kinase MAK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163106] [GtoPdb: 2061] [UniProtKB: P20794] | ||||||||
| ChEMBL | Binding constant for MAK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| microtubule affinity regulating kinase 1/Serine/threonine-protein kinase MARK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5940] [GtoPdb: 2097] [UniProtKB: Q9P0L2] | ||||||||
| ChEMBL | Binding constant for MARK1 kinase domain | B | 6.15 | pKd | 700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MARK2 kinase domain | B | 5.51 | pKd | 3100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MRCKA kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| CDC42 binding protein kinase beta/Serine/threonine-protein kinase MRCK beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5052] [GtoPdb: 1508] [UniProtKB: Q9Y5S2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for MRCKB kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| CDC42 binding protein kinase gamma/Serine/threonine-protein kinase MRCK gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5615] [GtoPdb: 1506] [UniProtKB: Q6DT37] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for DMPK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
| ChEMBL | Binding constant for MTOR kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase N1/Serine/threonine-protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PKN1 kinase domain | B | 5.96 | pKd | 1100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| protein kinase N2/Serine/threonine-protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PKN2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| NIMA related kinase 1/Serine/threonine-protein kinase Nek1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5855] [GtoPdb: 2114] [UniProtKB: Q96PY6] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for NEK1 kinase domain | B | 5.47 | pKd | 3400 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of NEK1 (unknown origin) assessed as dissociation constant | B | 5.47 | pKd | 3400 | nM | Kd | Medchemcomm (2018) 9: 44-66 [PMID:30108900] |
| NIMA related kinase 11/Serine/threonine-protein kinase Nek11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5638] [GtoPdb: 2116] [UniProtKB: Q8NG66] | ||||||||
| ChEMBL | Binding constant for NEK11 kinase domain | B | 5.92 | pKd | 1200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of NEK11 (unknown origin) assessed as dissociation constant | B | 5.92 | pKd | 1200 | nM | Kd | Medchemcomm (2018) 9: 44-66 [PMID:30108900] |
| NIMA related kinase 2/Serine/threonine-protein kinase Nek2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3835] [GtoPdb: 2117] [UniProtKB: P51955] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for NEK2 kinase domain | B | 5.77 | pKd | 1700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of NEK2 (unknown origin) assessed as dissociation constant | B | 5.77 | pKd | 1700 | nM | Kd | Medchemcomm (2018) 9: 44-66 [PMID:30108900] |
| NIMA related kinase 3/Serine/threonine-protein kinase Nek3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5679] [GtoPdb: 2118] [UniProtKB: P51956] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for NEK3 kinase domain | B | 6.19 | pKd | 640 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of NEK3 (unknown origin) assessed as dissociation constant | B | 6.19 | pKd | 640 | nM | Kd | Medchemcomm (2018) 9: 44-66 [PMID:30108900] |
| NIMA related kinase 4/Serine/threonine-protein kinase Nek4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5819] [GtoPdb: 2119] [UniProtKB: P51957] | ||||||||
| ChEMBL | Binding constant for NEK4 kinase domain | B | 5.8 | pKd | 1600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of NEK4 (unknown origin) assessed as dissociation constant | B | 5.8 | pKd | 1600 | nM | Kd | Medchemcomm (2018) 9: 44-66 [PMID:30108900] |
| NIMA related kinase 5/Serine/threonine-protein kinase Nek5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5044] [GtoPdb: 2120] [UniProtKB: Q6P3R8] | ||||||||
| ChEMBL | Binding constant for NEK5 kinase domain | B | 6.24 | pKd | 570 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of NEK5 (unknown origin) assessed as dissociation constant | B | 6.24 | pKd | 570 | nM | Kd | Medchemcomm (2018) 9: 44-66 [PMID:30108900] |
| NIMA related kinase 6/Serine/threonine-protein kinase Nek6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98] | ||||||||
| ChEMBL | Binding constant for NEK6 kinase domain | B | 6.92 | pKd | 120 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of NEK6 (unknown origin) assessed as dissociation constant | B | 6.92 | pKd | 120 | nM | Kd | Medchemcomm (2018) 9: 44-66 [PMID:30108900] |
| NIMA related kinase 7/Serine/threonine-protein kinase Nek7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4849] [GtoPdb: 2122] [UniProtKB: Q8TDX7] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for NEK7 kinase domain | B | 6.8 | pKd | 160 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of NEK7 (unknown origin) assessed as dissociation constant | B | 6.8 | pKd | 160 | nM | Kd | Medchemcomm (2018) 9: 44-66 [PMID:30108900] |
| NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.79 | pKd | 1634 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for NEK9 kinase domain | B | 6.82 | pKd | 150 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of NEK9 (unknown origin) assessed as dissociation constant | B | 6.82 | pKd | 150 | nM | Kd | Medchemcomm (2018) 9: 44-66 [PMID:30108900] |
| serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84] | ||||||||
| ChEMBL | Binding constant for NIM1 kinase domain | B | 5.36 | pKd | 4400 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| nemo like kinase/Serine/threonine-protein kinase NLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8] | ||||||||
| ChEMBL | Binding constant for NLK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| oxidative stress responsive kinase 1/Serine/threonine-protein kinase OSR1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163104] [GtoPdb: 2132] [UniProtKB: O95747] | ||||||||
| ChEMBL | Binding constant for OSR1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4600] [GtoPdb: 2133] [UniProtKB: Q13153] | ||||||||
| ChEMBL | Binding constant for PAK1 kinase domain | B | 5.51 | pKd | 3100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PAK2 kinase domain | B | 5.22 | pKd | 6000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| p21 (RAC1) activated kinase 3/Serine/threonine-protein kinase PAK 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2999] [GtoPdb: 2135] [UniProtKB: O75914] | ||||||||
| ChEMBL | Binding constant for PAK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PAK4 kinase domain | B | 5.42 | pKd | 3800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| p21 (RAC1) activated kinase 5/Serine/threonine-protein kinase PAK 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4524] [GtoPdb: 2138] [UniProtKB: Q9P286] | ||||||||
| ChEMBL | Binding constant for PAK7 kinase domain | B | 5.92 | pKd | 1200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5] | ||||||||
| ChEMBL | Binding constant for PAK6 kinase domain | B | 5.16 | pKd | 6900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PIM1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| ChEMBL | Binding constant for PIM2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86] | ||||||||
| ChEMBL | Binding constant for PIM3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Serine/threonine-protein kinase PknB in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908385] [UniProtKB: P9WI81] | ||||||||
| ChEMBL | Binding constant for PKNB(M.tuberculosis) kinase domain | B | 7 | pKd | 100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PLK1 kinase domain | B | 6.55 | pKd | 280 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3] | ||||||||
| ChEMBL | Binding constant for PLK2 kinase domain | B | 5.62 | pKd | 2400 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4] | ||||||||
| ChEMBL | Binding constant for PLK3 kinase domain | B | 5.8 | pKd | 1600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.71 | pKd | 1954 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for PLK4 kinase domain | B | 7.02 | pKd | 96 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| pre-mRNA processing factor kinase PRP4K/Serine/threonine-protein kinase PRP4 homolog in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908382] [GtoPdb: 2177] [UniProtKB: Q13523] | ||||||||
| ChEMBL | Binding constant for PRP4 kinase domain | B | 6.41 | pKd | 390 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| RIO kinase 1/Serine/threonine-protein kinase RIO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5975] [GtoPdb: 2186] [UniProtKB: Q9BRS2] | ||||||||
| ChEMBL | Binding constant for RIOK1 kinase domain | B | 7 | pKd | 100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| RIO kinase 2/Serine/threonine-protein kinase RIO2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6000] [GtoPdb: 2187] [UniProtKB: Q9BVS4] | ||||||||
| ChEMBL | Binding constant for RIOK2 kinase domain | B | 5.59 | pKd | 2600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| RIO kinase 3/Serine/threonine-protein kinase RIO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5659] [GtoPdb: 2188] [UniProtKB: O14730] | ||||||||
| ChEMBL | Binding affinity to RIOK3 (unknown origin) | B | 7 | pKd | 100 | nM | Kd | US-20200216545-A1. Compositions and methods for treating beta-globinopathies (2020) |
| ChEMBL | Binding constant for RIOK3 kinase domain | B | 7.04 | pKd | 91 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding affinity to RIOK3 (unknown origin) | B | 7.04 | pKd | 91 | nM | Kd | US-20200216545-A1. Compositions and methods for treating beta-globinopathies (2020) |
| SH3 domain binding kinase 1/Serine/threonine-protein kinase SBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163129] [GtoPdb: 2193] [UniProtKB: Q52WX2] | ||||||||
| ChEMBL | Binding constant for SBK1 kinase domain | B | 6.1 | pKd | 790 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serum/glucocorticoid regulated kinase family member 3/Serine/threonine-protein kinase Sgk3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6186] [GtoPdb: 1536] [UniProtKB: Q96BR1] | ||||||||
| ChEMBL | Binding constant for SGK3 kinase domain | B | 5.6 | pKd | 2500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| salt inducible kinase 1/Serine/threonine-protein kinase SIK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6082] [GtoPdb: 2197] [UniProtKB: P57059] | ||||||||
| ChEMBL | Binding constant for SIK kinase domain | B | 7.41 | pKd | 39 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| salt inducible kinase 2/Serine/threonine-protein kinase SIK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5699] [GtoPdb: 2198] [UniProtKB: Q9H0K1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6 | pKd | 1008 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for SIK2 kinase domain | B | 7.01 | pKd | 98 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| SIK family kinase 3/Serine/threonine-protein kinase SIK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6149] [GtoPdb: 2199] [UniProtKB: Q9Y2K2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for QSK kinase domain | B | 5.72 | pKd | 1900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| serine/threonine kinase 11/Serine/threonine-protein kinase STK11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5606] [GtoPdb: 2212] [UniProtKB: Q15831] | ||||||||
| ChEMBL | Binding constant for LKB1 kinase domain | B | 6.51 | pKd | 310 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for TAOK1 kinase domain | B | 5.89 | pKd | 1300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for TAOK2 kinase domain | B | 6.12 | pKd | 760 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for TAOK3 kinase domain | B | 5.72 | pKd | 1900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.65 | pKd | 2230 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for TBK1 kinase domain | B | 7.04 | pKd | 92 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TNNI3 interacting kinase/Serine/threonine-protein kinase TNNI3K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5260] [GtoPdb: 2247] [UniProtKB: Q59H18] | ||||||||
| ChEMBL | Binding constant for TNNI3K kinase domain | B | 5.74 | pKd | 1800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| tousled like kinase 1/Serine/threonine-protein kinase tousled-like 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5388] [GtoPdb: 2242] [UniProtKB: Q9UKI8] | ||||||||
| ChEMBL | Binding constant for TLK1 kinase domain | B | 5.89 | pKd | 1300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| tousled like kinase 2/Serine/threonine-protein kinase tousled-like 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5404] [GtoPdb: 2243] [UniProtKB: Q86UE8] | ||||||||
| ChEMBL | Binding constant for TLK2 kinase domain | B | 5.7 | pKd | 2000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ULK1 kinase domain | B | 6.57 | pKd | 270 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| unc-51 like autophagy activating kinase 2/Serine/threonine-protein kinase ULK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5435] [GtoPdb: 2272] [UniProtKB: Q8IYT8] | ||||||||
| ChEMBL | Binding constant for ULK2 kinase domain | B | 7.1 | pKd | 79 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| unc-51 like kinase 3/Serine/threonine-protein kinase ULK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5047] [GtoPdb: 2273] [UniProtKB: Q6PHR2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ULK3 kinase domain | B | 6.54 | pKd | 290 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| VRK serine/threonine kinase 2/Serine/threonine-protein kinase VRK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649059] [GtoPdb: 2276] [UniProtKB: Q86Y07] | ||||||||
| ChEMBL | Binding constant for VRK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Signal recognition particle receptor subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105934] [UniProtKB: P08240] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| SNF related kinase/SNF-related serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908384] [GtoPdb: 2202] [UniProtKB: Q9NRH2] | ||||||||
| ChEMBL | Binding constant for SNRK kinase domain | B | 6.64 | pKd | 230 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| SRSF protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4375] [GtoPdb: 2208] [UniProtKB: Q96SB4] | ||||||||
| ChEMBL | Binding constant for SRPK1 kinase domain | B | 6.8 | pKd | 160 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| SRSF protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5668] [GtoPdb: 2209] [UniProtKB: P78362] | ||||||||
| ChEMBL | Binding constant for SRPK2 kinase domain | B | 7 | pKd | 100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| SRSF protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5415] [GtoPdb: 2210] [UniProtKB: Q9UPE1] | ||||||||
| ChEMBL | Binding constant for SRPK3 kinase domain | B | 6.77 | pKd | 170 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| STE20 like kinase/STE20-like serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for SLK kinase domain | B | 6.17 | pKd | 680 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| STE20 related adaptor alpha/STE20-related kinase adapter protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795198] [GtoPdb: 2227] [UniProtKB: Q7RTN6] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 39/STE20/SPS1-related proline-alanine-rich protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163108] [GtoPdb: 2224] [UniProtKB: Q9UEW8] | ||||||||
| ChEMBL | Binding constant for STK39 kinase domain | B | 5.8 | pKd | 1600 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Structural maintenance of chromosomes protein 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105747] [UniProtKB: Q14683] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Structural maintenance of chromosomes protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105890] [UniProtKB: O95347] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105973] [UniProtKB: Q9P2R7] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| testis specific serine kinase 1B/Testis-specific serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6003] [GtoPdb: 2257] [UniProtKB: Q9BXA7] | ||||||||
| ChEMBL | Binding constant for TSSK1B kinase domain | B | 5.89 | pKd | 1300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for TGFBR1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| transforming growth factor beta receptor 2/TGF-beta receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173] | ||||||||
| ChEMBL | Binding constant for TGFBR2 kinase domain | B | 5.96 | pKd | 1100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Thyroid hormone receptor-associated protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105820] [UniProtKB: Q9Y2W1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TRAF2 and NCK interacting kinase/TRAF2 and NCK-interacting protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for TNIK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TRPM6/Transient receptor potential cation channel subfamily M member 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628470] [GtoPdb: 498] [UniProtKB: Q9BX84] | ||||||||
| ChEMBL | Binding constant for TRPM6 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ABL1(F317I)-non phosphorylated kinase domain | B | 5.68 | pKd | 2100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(F317I)-phosphorylated kinase domain | B | 6.25 | pKd | 560 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(F317L)-non phosphorylated kinase domain | B | 6.35 | pKd | 450 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(T315I)-non phosphorylated kinase domain | B | 6.62 | pKd | 240 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(F317L)-phosphorylated kinase domain | B | 6.74 | pKd | 180 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1-non phosphorylated kinase domain | B | 6.74 | pKd | 180 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(Q252H)-non phosphorylated kinase domain | B | 6.96 | pKd | 110 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(T315I)-phosphorylated kinase domain | B | 7.19 | pKd | 65 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(H396P)-phosphorylated kinase domain | B | 7.21 | pKd | 61 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | B | 7.25 | pKd | 56 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | B | 7.27 | pKd | 54 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(M351T)-phosphorylated kinase domain | B | 7.3 | pKd | 50 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(H396P)-non phosphorylated kinase domain | B | 7.35 | pKd | 45 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1-phosphorylated kinase domain | B | 7.36 | pKd | 44 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding constant for ABL1(E255K)-phosphorylated kinase domain | B | 7.4 | pKd | 40 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ABL proto-oncogene 2, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4014] [GtoPdb: 1924] [UniProtKB: P42684] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for ABL2 kinase domain | B | 6.24 | pKd | 570 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Blk in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451] | ||||||||
| ChEMBL | Binding constant for BLK kinase domain | B | 6.19 | pKd | 650 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for BTK kinase domain | B | 6.07 | pKd | 850 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for CSK kinase domain | B | 5.23 | pKd | 5900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| FER tyrosine kinase/Tyrosine-protein kinase Fer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for FER kinase domain | B | 5.96 | pKd | 1100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Fes/Fps in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for FES kinase domain | B | 6.28 | pKd | 530 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fgr in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] | ||||||||
| ChEMBL | Binding constant for FGR kinase domain | B | 7.09 | pKd | 82 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for FRK kinase domain | B | 6.7 | pKd | 200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for FYN kinase domain | B | 7.42 | pKd | 38 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for HCK kinase domain | B | 5.68 | pKd | 2100 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881] | ||||||||
| ChEMBL | Binding constant for ITK kinase domain | B | 6.31 | pKd | 490 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | B | 5.7 | pKd | 2000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Binding affinity to recombinant human JAK1 kinase domain by fluorescence polarization assay | B | 6.59 | pKd | 258 | nM | Kd | J Med Chem (2024) 67: 10012-10024 [PMID:38843875] |
| ChEMBL | Binding constant for JAK1(JH1domain-catalytic) kinase domain | B | 7.74 | pKd | 18 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of human JAK1 | B | 6.98 | pKi | 105 | nM | Ki | J Med Chem (2018) 61: 9030-9058 [PMID:29870256] |
| GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7454-7 [PMID:21106455] |
| ChEMBL | Inhibition of human recombinant JAK1 by TR-FRET assay | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7454-7457 [PMID:21106455] |
| ChEMBL | Inhibition of recombinant human JAK1 assessed as inhibition of substrate phosphorylation measured every 5 mins for 30 mins by LANCE Ultra kinase assay | B | 7.25 | pIC50 | 56 | nM | IC50 | J Med Chem (2024) 67: 10012-10024 [PMID:38843875] |
| ChEMBL | Inhibition of JAK1 (unknown origin) | B | 7.68 | pIC50 | 20.75 | nM | IC50 | J Med Chem (2023) 66: 5753-5773 [PMID:37057760] |
| ChEMBL | Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s). | B | 7.7 | pIC50 | 20 | nM | IC50 | US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018) |
| ChEMBL | Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. | B | 7.7 | pIC50 | 20 | nM | IC50 | US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020) |
| ChEMBL | Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. | B | 7.7 | pIC50 | 20 | nM | IC50 | US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021) |
| ChEMBL | Inhibition of JAK1 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescent assay | B | 7.91 | pIC50 | 12.3 | nM | IC50 | J Med Chem (2023) 66: 14150-14174 [PMID:37796543] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Binding affinity to recombinant human JAK2 kinase domain by fluorescence polarization assay | B | 8.37 | pKd | 4.3 | nM | Kd | J Med Chem (2024) 67: 10012-10024 [PMID:38843875] |
| ChEMBL | Binding constant for JAK2(JH1domain-catalytic) kinase domain | B | 8.96 | pKd | 1.1 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of JAK-2 in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.18 | pIC50 | 6607.9 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK2V617F in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.18 | pIC50 | 6607.9 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK2V617F in human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.75 | pIC50 | 1779.3 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK-2 in human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.75 | pIC50 | 1779.3 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK2V617F in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.78 | pIC50 | 1660.6 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK-2 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.78 | pIC50 | 1660.6 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK2 in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.83 | pIC50 | 1469.5 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK2-V617F mutant in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.83 | pIC50 | 1469.5 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK-2 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.95 | pIC50 | 1123 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK2V617F in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5.95 | pIC50 | 1123 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK2-mediated erythropoietin-induced STAT5 phosphorylation in human TF-1 cells pretreated for 60 mins followed by erythropoietin addition and measured after 15 mins by pacific orange/pacific blue NHS esters based Beckmann coulter flow cytometer | B | 6.34 | pIC50 | 457 | nM | IC50 | J Med Chem (2024) 67: 10012-10024 [PMID:38843875] |
| ChEMBL | Inhibition of JAK-2 in Melphalan Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6.42 | pIC50 | 381.2 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK2V617F in Melphalan Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6.42 | pIC50 | 381.2 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of JAK2 (unknown origin) incubated for 30 mins in presence of ATP by HTRF assay | B | 7.91 | pIC50 | 12.24 | nM | IC50 | J Med Chem (2023) 66: 5753-5773 [PMID:37057760] |
| ChEMBL | Inhibition of recombinant human JAK2 assessed as inhibition of substrate phosphorylation measured every 5 mins for 30 mins by LANCE Ultra kinase assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2024) 67: 10012-10024 [PMID:38843875] |
| ChEMBL | Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s). | B | 8.1 | pIC50 | 8 | nM | IC50 | US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018) |
| ChEMBL | Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. | B | 8.1 | pIC50 | 8 | nM | IC50 | US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020) |
| ChEMBL | Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. | B | 8.1 | pIC50 | 8 | nM | IC50 | US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021) |
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
| ChEMBL | Kinase Assay: JAK2 and JAK2 [V617F] Kinase Assay: In 5Ă— Kinase Buffer A, JAK2 or JAK2 [V617F] kinase was mixed with pre-diluted compounds at different concentrations in duplicate for 10 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 20 minutes (in which negative and positive controls were set: the negative control was a blank control and the positive control was erlotinib). After the reaction was completed, a detection reagent (the reagent in the HTRF Kinase TK kit) was added. After incubation at room temperature for 30 minutes, the enzyme activities in the presence of the compounds disclosed herein at each concentration were measured by an Evnvision microplate reader, and inhibitory activities of compounds at different concentrations on the enzyme activity were calculated. The inhibitory activities of compounds at different concentrations on enzyme activity were then fitted according to the four-parameter equation using Graphpad 5.0 software, and the IC50 values were calculated. | B | 8.46 | pIC50 | 3.47 | nM | IC50 | US-11384069-B2. Diphenylaminopyrimidine compound for inhibiting kinase activity (2022) |
| ChEMBL | Kinase Assay: JAK2 and JAK2 [V617F] Kinase Assay: In 5Ă— Kinase Buffer A, JAK2 or JAK2 [V617F] kinase was mixed with pre-diluted compounds at different concentrations in duplicate for 10 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 20 minutes (in which negative and positive controls were set: the negative control was a blank control and the positive control was erlotinib). After the reaction was completed, a detection reagent (the reagent in the HTRF Kinase TK kit) was added. After incubation at room temperature for 30 minutes, the enzyme activities in the presence of the compounds disclosed herein at each concentration were measured by an Evnvision microplate reader, and inhibitory activities of compounds at different concentrations on the enzyme activity were calculated. The inhibitory activities of compounds at different concentrations on enzyme activity were then fitted according to the four-parameter equation using Graphpad 5.0 software, and the IC50 values were calculated. | B | 8.49 | pIC50 | 3.24 | nM | IC50 | US-11384069-B2. Diphenylaminopyrimidine compound for inhibiting kinase activity (2022) |
| ChEMBL | Inhibition of JAK2 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescent assay | B | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2023) 66: 14150-14174 [PMID:37796543] |
| ChEMBL | Kinase Assay: JAK2 and JAK2 [V617F] Kinase Assay: In 5Ă— Kinase Buffer A, JAK2 or JAK2 [V617F] kinase was mixed with pre-diluted compounds at different concentrations in duplicate for 10 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 20 minutes (in which negative and positive controls were set: the negative control was a blank control and the positive control was erlotinib). After the reaction was completed, a detection reagent (the reagent in the HTRF Kinase TK kit) was added. After incubation at room temperature for 30 minutes, the enzyme activities in the presence of the compounds disclosed herein at each concentration were measured by an Evnvision microplate reader, and inhibitory activities of compounds at different concentrations on the enzyme activity were calculated. The inhibitory activities of compounds at different concentrations on enzyme activity were then fitted according to the four-parameter equation using Graphpad 5.0 software, and the IC50 values were calculated. | B | 8.5 | pIC50 | 3.16 | nM | IC50 | US-11384069-B2. Diphenylaminopyrimidine compound for inhibiting kinase activity (2022) |
| ChEMBL | Kinase Assay: JAK2 and JAK2 [V617F] Kinase Assay: In 5Ă— Kinase Buffer A, JAK2 or JAK2 [V617F] kinase was mixed with pre-diluted compounds at different concentrations in duplicate for 10 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 20 minutes (in which negative and positive controls were set: the negative control was a blank control and the positive control was erlotinib). After the reaction was completed, a detection reagent (the reagent in the HTRF Kinase TK kit) was added. After incubation at room temperature for 30 minutes, the enzyme activities in the presence of the compounds disclosed herein at each concentration were measured by an Evnvision microplate reader, and inhibitory activities of compounds at different concentrations on the enzyme activity were calculated. The inhibitory activities of compounds at different concentrations on enzyme activity were then fitted according to the four-parameter equation using Graphpad 5.0 software, and the IC50 values were calculated. | B | 8.51 | pIC50 | 3.08 | nM | IC50 | US-11384069-B2. Diphenylaminopyrimidine compound for inhibiting kinase activity (2022) |
| ChEMBL | Kinase Assay: JAK2 and JAK2 [V617F] Kinase Assay: In 5Ă— Kinase Buffer A, JAK2 or JAK2 [V617F] kinase was mixed with pre-diluted compounds at different concentrations in duplicate for 10 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 20 minutes (in which negative and positive controls were set: the negative control was a blank control and the positive control was erlotinib). After the reaction was completed, a detection reagent (the reagent in the HTRF Kinase TK kit) was added. After incubation at room temperature for 30 minutes, the enzyme activities in the presence of the compounds disclosed herein at each concentration were measured by an Evnvision microplate reader, and inhibitory activities of compounds at different concentrations on the enzyme activity were calculated. The inhibitory activities of compounds at different concentrations on enzyme activity were then fitted according to the four-parameter equation using Graphpad 5.0 software, and the IC50 values were calculated. | B | 8.51 | pIC50 | 3.06 | nM | IC50 | US-11384069-B2. Diphenylaminopyrimidine compound for inhibiting kinase activity (2022) |
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 |
Bioorg Med Chem Lett (2010) 20: 7454-7 [PMID:21106455]; Cancer Cell (2008) 13: 311-20 [PMID:18394554] |
| ChEMBL | Inhibition of JAK2 V617F mutant (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986] |
| ChEMBL | Inhibition of wild-type JAK2 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986] |
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325] |
| ChEMBL | Inhibition of JAK 2 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2021) 64: 2-25 [PMID:33356242] |
| ChEMBL | Inhibition of human JAK2 | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2018) 61: 9030-9058 [PMID:29870256] |
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Medchemcomm (2012) 3: 22-27 |
| ChEMBL | Inhibition of human recombinant JAK2 by TR-FRET assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7454-7457 [PMID:21106455] |
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2024) 275: 116540-116540 [PMID:38852338] |
| ChEMBL | Inhibition of JAK2 (unknown origin) incubated for 30 mins in presence of ATP by HTRF assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2023) 260: 115762-115762 [PMID:37683364] |
| ChEMBL | Inhibition of JAK2 V617F mutant (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2023) 261: 115848-115848 [PMID:37793326] |
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2023) 66: 5753-5773 [PMID:37057760] |
| ChEMBL | Inhibition of GST tagged JAK2 (unknown origin) expressed in insect cells | B | 8.52 | pIC50 | 3 | nM | IC50 | Leukemia (2009) 23: 1441-1445 [PMID:19295546] |
| ChEMBL | Kinase Assay: JAK2 and JAK2 [V617F] Kinase Assay: In 5Ă— Kinase Buffer A, JAK2 or JAK2 [V617F] kinase was mixed with pre-diluted compounds at different concentrations in duplicate for 10 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 20 minutes (in which negative and positive controls were set: the negative control was a blank control and the positive control was erlotinib). After the reaction was completed, a detection reagent (the reagent in the HTRF Kinase TK kit) was added. After incubation at room temperature for 30 minutes, the enzyme activities in the presence of the compounds disclosed herein at each concentration were measured by an Evnvision microplate reader, and inhibitory activities of compounds at different concentrations on the enzyme activity were calculated. The inhibitory activities of compounds at different concentrations on enzyme activity were then fitted according to the four-parameter equation using Graphpad 5.0 software, and the IC50 values were calculated. | B | 8.54 | pIC50 | 2.89 | nM | IC50 | US-11384069-B2. Diphenylaminopyrimidine compound for inhibiting kinase activity (2022) |
| ChEMBL | Inhibition of human JAK2 by radiometric assay | B | 9.12 | pIC50 | 0.75 | nM | IC50 | J Med Chem (2021) 64: 2228-2241 [PMID:33570945] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Binding affinity to recombinant human JAK3 kinase domain by fluorescence polarization assay | B | 7.07 | pKd | 85 | nM | Kd | J Med Chem (2024) 67: 10012-10024 [PMID:38843875] |
| ChEMBL | Binding constant for JAK3(JH1domain-catalytic) kinase domain | B | 7.13 | pKd | 74 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| ChEMBL | Inhibition of human JAK3 | B | 6 | pKi | 1002 | nM | Ki | J Med Chem (2018) 61: 9030-9058 [PMID:29870256] |
| ChEMBL | Inhibition of recombinant human JAK3 assessed as inhibition of substrate phosphorylation measured every 5 mins for 30 mins by LANCE Ultra kinase assay | B | 5.74 | pIC50 | 1812 | nM | IC50 | J Med Chem (2024) 67: 10012-10024 [PMID:38843875] |
| ChEMBL | Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. | B | 5.82 | pIC50 | 1500 | nM | IC50 | US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021) |
| ChEMBL | Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s). | B | 5.82 | pIC50 | 1500 | nM | IC50 | US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018) |
| ChEMBL | Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. | B | 5.82 | pIC50 | 1500 | nM | IC50 | US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020) |
| GtoPdb | - | - | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7454-7 [PMID:21106455] |
| ChEMBL | Inhibition of human recombinant JAK3 by TR-FRET assay | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7454-7457 [PMID:21106455] |
| ChEMBL | Inhibition of JAK3 (unknown origin) | B | 6.51 | pIC50 | 311.5 | nM | IC50 | J Med Chem (2023) 66: 5753-5773 [PMID:37057760] |
| ChEMBL | Inhibition of JAK3 (unknown origin) incubated for 40 mins in presence of ATP by Kinase-glo luminescent assay | B | 6.63 | pIC50 | 236 | nM | IC50 | J Med Chem (2023) 66: 14150-14174 [PMID:37796543] |
| ChEMBL | Inhibition of JAK3 (unknown origin) | B | 6.77 | pIC50 | 169 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for LCK kinase domain | B | 7.14 | pKd | 72 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for LYN kinase domain | B | 6.3 | pKd | 500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| ChEMBL | Binding constant for MERTK kinase domain | B | 6.09 | pKd | 820 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| tyrosine kinase with immunoglobulin like and EGF like domains 1/Tyrosine-protein kinase receptor Tie-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5274] [GtoPdb: 1841] [UniProtKB: P35590] | ||||||||
| ChEMBL | Binding constant for TIE1 kinase domain | B | 6.15 | pKd | 700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TYRO3 protein tyrosine kinase/Tyrosine-protein kinase receptor TYRO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5314] [GtoPdb: 1836] [UniProtKB: Q06418] | ||||||||
| ChEMBL | Binding constant for TYRO3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Binding constant for AXL kinase domain | B | 6.8 | pKd | 160 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites/Tyrosine-protein kinase Srms in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5703] [GtoPdb: 2207] [UniProtKB: Q9H3Y6] | ||||||||
| ChEMBL | Binding constant for SRMS kinase domain | B | 5.3 | pKd | 5000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for SYK kinase domain | B | 5.57 | pKd | 2700 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| tec protein tyrosine kinase/Tyrosine-protein kinase Tec in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for TEC kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681] | ||||||||
| ChEMBL | Binding constant for TXK kinase domain | B | 5.82 | pKd | 1500 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase Yes in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for YES kinase domain | B | 6.92 | pKd | 120 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Binding constant for ZAP70 kinase domain | B | 5.42 | pKd | 3800 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Tyrosine--tRNA ligase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3179] [UniProtKB: P54577] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| U5 small nuclear ribonucleoprotein 200 kDa helicase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105972] [UniProtKB: O75643] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| UMP-CMP kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5681] [UniProtKB: P30085] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Uncharacterized protein FLJ45252 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105933] [UniProtKB: Q6ZSR9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.56 | pKd | 277 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| sugen kinase 110/Uncharacterized serine/threonine-protein kinase SBK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5116] [GtoPdb: 2290] [UniProtKB: P0C264] | ||||||||
| ChEMBL | Binding constant for SgK110 kinase domain | B | 5.54 | pKd | 2900 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] | ||||||||
| ChEMBL | Binding constant for FLT1 kinase domain | B | 5.37 | pKd | 4300 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Binding constant for VEGFR2 kinase domain | B | 5.28 | pKd | 5200 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
| ChEMBL | Binding constant for FLT4 kinase domain | B | 5.7 | pKd | 2000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| Very long-chain specific acyl-CoA dehydrogenase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105892] [UniProtKB: P49748] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| WEE1 G2 checkpoint kinase/Wee1-like protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.71 | pKd | 1951 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding constant for WEE1 kinase domain | B | 6.41 | pKd | 390 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
| WEE2 oocyte meiosis inhibiting kinase/Wee1-like protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5095] [GtoPdb: 2279] [UniProtKB: P0C1S8] | ||||||||
| ChEMBL | Binding constant for WEE2 kinase domain | B | 5.22 | pKd | 6000 | nM | Kd | Nat Biotechnol (2011) 29: 1046-1051 [PMID:22037378] |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
