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| ChEMBL ligand: CHEMBL3301622 (Asp-2215, ASP-2215, ASP2215, Gilteritinib) |
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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] |
| 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] |
| 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 | 6.82 | pKd | 152 | 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 | 5.26 | pKd | 5511 | 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 | 5.5 | pKd | 3149 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 7.41 | pKd | 39 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| 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 | 6.35 | pKd | 451 | 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 | 6.31 | pKd | 495 | 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 | Inhibition Assay: A recombinant retrovirus was created from expression plasmid FLAG-EML4-ALKv1/pMX-iresCD8 in which cDNA for EMLA-ALK fusion protein v1 was integrated, and injected into mouse lymphoid cell line BA/F3 cells. Using a magnetic bead reagent for cell separation and a purification column (anti-CD8 monoclonal antibody immobilized on magnetic beads and a MiniMACS purification column; both are products of MilteDyi Biotec Inc.), cell surface CD8-expressing cells were purified to establish EML4-ALK fusion protein v1-expressing BA/F3 cells. From the cells, EML4-ALK fusion protein v1 was purified and subjected to kinase activity evaluation. EML4-ALK fusion protein v1 was investigated for its phosphorylation activity toward a peptide substrate by using a kinase activity detection kit (HTRF KinEASE-TK; Cisbio Inc.). Test compounds were each added to a reaction solution containing the enzyme protein to give 8 final concentrations from 1000 nM to 0.3 nM, followed by addition of ATP. | B | 8.82 | pIC50 | 1.5 | nM | IC50 | US-8969336-B2. Diamino heterocyclic carboxamide compound (2015) |
| ChEMBL | Inhibition of ALK (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2021) 64: 2878-2900 [PMID:33719439] |
| ChEMBL | Inhibition of ALK (unknown origin) in presence of ATP | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2021) 64: 2878-2900 [PMID:33719439] |
| GtoPdb | - | - | 9.3 | pIC50 | ~0.5 | nM | IC50 | Blood (2017) 129: 257-260 [PMID:27908881] |
| 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 | 7.6 | pKd | 25 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 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 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] |
| 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 | 6.74 | pKd | 184 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.26 | pKd | 5481 | 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 | 7.34 | pKd | 46 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.92 | pKd | 121 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.24 | pKd | 572 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.58 | pKd | 2648 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.68 | pKd | 207 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.77 | pKd | 169 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.38 | pKd | 421 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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, 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] |
| 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] |
| 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] |
| 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] |
| casein kinase 1 gamma 2/Casein kinase I isoform gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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 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] |
| 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 | 6.02 | pKd | 960 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613, P51946, P51948] | ||||||||
| ChEMBL | Inhibition of CDK7/cyclin H/MAT1 (unknown origin) using HYSPTSPSYSPTSPSYSPTSPSKKKK-O substrate incubated for 120 mins measured after 40 mins incubation under dark by ADP-glo based luminescence assay | B | 5.3 | pKi | >5000 | nM | Ki | Eur J Med Chem (2021) 213: 113215-113215 [PMID:33516985] |
| 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] |
| 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 | 5.63 | pKd | 2346 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 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] |
| 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] |
| 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] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
| ChEMBL | Inhibition of CDK1/cyclin B (unknown origin) using histone 1 protein substrate incubated for 120 mins measured after 40 mins incubation under dark by ADP-glo based luminescence assay | B | 5.3 | pKi | >5000 | nM | Ki | Eur J Med Chem (2021) 213: 113215-113215 [PMID:33516985] |
| 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] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] | ||||||||
| ChEMBL | Inhibition of CDK2/cyclin E (unknown origin) using histone 1 protein substrate incubated for 120 mins measured after 40 mins incubation under dark by ADP-glo based luminescence assay | B | 5.83 | pKi | 1485 | nM | Ki | Eur J Med Chem (2021) 213: 113215-113215 [PMID:33516985] |
| 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] |
| 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 | 5.71 | pKd | 1955 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| cyclin-dependent kinase like 5/Cyclin-dependent kinase-like 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163112] [GtoPdb: 1986] [UniProtKB: O76039] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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 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 | 8.05 | pKd | 9 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.69 | pKd | 202 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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 | 6.36 | pKd | 432 | 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] |
| 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] |
| 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 | 5.56 | pKd | 2755 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.3 | pKd | 502 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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 | 5.69 | pKd | 2040 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.72 | pKd | 1895 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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 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 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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 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] |
| 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] |
| 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 | 5.57 | pKd | 2716 | 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 | 6.33 | pKd | 464 | 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] |
| 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] |
| 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] |
| 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] |
| EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.53 | pKd | 2980 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| 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 | 6.62 | pKd | 241 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.46 | pKd | 3502 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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 | 6.12 | pKd | 759 | 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] |
| Guanine nucleotide-binding protein G(i) subunit alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105887] [UniProtKB: P04899] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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] |
| neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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] |
| GtoPdb | - | - | 8.96 | pIC50 | ~1.1 | nM | IC50 | Blood (2017) 129: 257-260 [PMID:27908881] |
| 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 | 5.83 | pKd | 1468 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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 | 8.15 | pKd | 7 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.76 | pKd | 1757 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376] | ||||||||
| ChEMBL | Inhibition of LTK (unknown origin) in presence of ATP | B | 9.46 | pIC50 | 0.35 | nM | IC50 | J Med Chem (2021) 64: 2878-2900 [PMID:33719439] |
| GtoPdb | - | - | 9.7 | pIC50 | ~0.2 | nM | IC50 | Blood (2017) 129: 257-260 [PMID:27908881] |
| 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] |
| 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] |
| Long-chain-fatty-acid--CoA ligase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105818] [UniProtKB: Q9ULC5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.68 | pKd | 208 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.09 | pKd | 804 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| Midasin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105779] [UniProtKB: Q9NU22] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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] |
| 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] |
| 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 | 6.29 | pKd | 512 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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 | 6.58 | pKd | 263 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.13 | pKd | 736 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.37 | pKd | 430 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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 | 6.22 | pKd | 600 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.27 | pKd | 536 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.97 | pKd | 108 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.61 | pKd | 244 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.22 | pKd | 605 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.69 | pKd | 202 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.51 | pKd | 3115 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.72 | pKd | 191 | 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 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] |
| 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 | 6.73 | pKd | 188 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 7.41 | pKd | 39 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| 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 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] |
| 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 | 7.32 | pKd | 48 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.29 | pKd | 510 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 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 | 6.23 | pKd | 591 | 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] |
| 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] |
| 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 | 6.29 | pKd | 510 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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 | 7.3 | pKd | 50 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition Assay: A partial protein of only a kinase domain of RET protein was purchased from Carna Biosciences Inc., Japan. The phosphorylation activity toward a peptide substrate was investigated using an EZ reader (Caliper). Test compounds were each mixed with a protein solution to give 8 final concentrations from 100 nM to 0.03 nM, followed by addition of a mixed liquid of ATP and substrate peptide (Caliper) and reaction for 30 minutes. The ATP concentration used was 100 µM. A reaction liquid which contained protein but no test compound (in which the solvent DMSO alone was added at 0.8% in place of the test compound) was prepared, followed by reaction in the same manner with or without ATP addition. In the absence of the test compound, the phosphorylation peptide peak without ATP addition and with ATP addition was assumed to be 100% inhibition and 0% inhibition, respectively. | B | 8.47 | pIC50 | 3.4 | nM | IC50 | US-8969336-B2. Diamino heterocyclic carboxamide compound (2015) |
| GtoPdb | - | - | 8.77 | pIC50 | ~1.7 | nM | IC50 | Blood (2017) 129: 257-260 [PMID:27908881] |
| 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 | Inhibition Assay: A partial protein of only a kinase domain of ROS protein was purchased from Carna Biosciences Inc., Japan, and tests were conducted as in Test Example 5, except that the ATP concentration in the mixed solution of ATP and substrate peptide (Caliper) was 50 uM. Test Example 5: A partial protein of only a kinase domain of RET protein was purchased from Carna Biosciences Inc., Japan. The phosphorylation activity toward a peptide substrate was investigated using an EZ reader (Caliper). Test compounds were each mixed with a protein solution to give 8 final concentrations from 100 nM to 0.03 nM, followed by addition of a mixed liquid of ATP and substrate peptide (Caliper) and reaction for 30 minutes. The ATP concentration used was 100 µM. A reaction liquid which contained protein but no test compound (in which the solvent DMSO alone was added at 0.8% in place of the test compound) was prepared, followed by reaction in the same manner with or without ATP addition. | B | 8.72 | pIC50 | 1.9 | nM | IC50 | US-8969336-B2. Diamino heterocyclic carboxamide compound (2015) |
| GtoPdb | - | - | 8.82 | pIC50 | ~1.5 | nM | IC50 | Blood (2017) 129: 257-260 [PMID:27908881] |
| 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] |
| 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 | 5.32 | pKd | 4830 | 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] |
| 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] |
| 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] |
| Ras-related C3 botulinum toxin substrate 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6094] [UniProtKB: P63000] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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-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 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 | 6.32 | pKd | 482 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.88 | pKd | 1304 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 8.15 | pKd | 7 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of wild type FLT3 (unknown origin) using Glu/Tyr peptide substrate incubated for 120 mins measured after 40 mins incubation under dark by ADP-glo based luminescence assay | B | 8 | pKi | 10 | nM | Ki | Eur J Med Chem (2021) 213: 113215-113215 [PMID:33516985] |
| ChEMBL | Inhibition of FLT3 ITD mutant (unknown origin) using Glu/Tyr peptide substrate incubated for 120 mins measured after 40 mins incubation under dark by ADP-glo based luminescence assay | B | 8.7 | pKi | 2 | nM | Ki | Eur J Med Chem (2021) 213: 113215-113215 [PMID:33516985] |
| ChEMBL | Inhibition of FLT3 (unknown origin) using MBP as substrate incubated for 40 mins in presence of ATP by ADP-Glo assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Nat Prod (2021) 84: 110-119 [PMID:33356258] |
| ChEMBL | Inhibition of FLT3 ITD mutant (unknown origin) | B | 6.93 | pIC50 | 117 | nM | IC50 | J Med Chem (2024) 67: 14702-14722 [PMID:39143914] |
| ChEMBL | Inhibition of FLT3 D835Y mutant (unknown origin) | B | 7.5 | pIC50 | 31.5 | nM | IC50 | J Med Chem (2024) 67: 14702-14722 [PMID:39143914] |
| ChEMBL | Inhibition of recombinant human FLT3-ITD mutant expressed in Sf9 insect cells using AGLT peptide and ATP as substrate in presence of [gamma-33P]ATP as substrate by radiometric assay | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2023) 66: 11133-11157 [PMID:37535845] |
| ChEMBL | Inhibition of wild type FLT3 (unknown origin) | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2023) 96: 129519-129519 [PMID:37838343] |
| ChEMBL | Inhibition of FLT3 (unknown origin) by bioluminescent ADP-Glo assay | B | 7.98 | pIC50 | 10.59 | nM | IC50 | Eur J Med Chem (2024) 264: 115977-115977 [PMID:38056299] |
| ChEMBL | Inhibition of recombinant human FLT3-ITD-F691L mutant expressed in Sf9 insect cells using myelin basic protein and ATP as substrate in presence of [gamma-33P]ATP as substrate by radiometric assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2023) 66: 11133-11157 [PMID:37535845] |
| ChEMBL | Inhibition of FLT3 D835Y mutant (unknown origin) | B | 8.11 | pIC50 | 7.7 | nM | IC50 | Bioorg Med Chem Lett (2023) 96: 129519-129519 [PMID:37838343] |
| ChEMBL | Inhibition of wild type FLT3 (unknown origin) phosphorylation in human SEMK2 cells | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2020) 63: 12403-12428 [PMID:32659083] |
| ChEMBL | Inhibition of recombinant FLT3 D835Y mutant (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay | B | 8.69 | pIC50 | 2.02 | nM | IC50 | Eur J Med Chem (2023) 262: 115860-115860 [PMID:37866334] |
| ChEMBL | Inhibition of recombinant human FLT3-D835Y mutant expressed in Sf9 insect cells using AGLT peptide and ATP as substrate in presence of [gamma-33P]ATP as substrate by radiometric assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2023) 66: 11133-11157 [PMID:37535845] |
| ChEMBL | Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay | B | 8.73 | pIC50 | 1.86 | nM | IC50 | Eur J Med Chem (2023) 262: 115860-115860 [PMID:37866334] |
| ChEMBL | Inhibition of FLT3 ITD mutant (unknown origin) using MBP as substrate incubated for 2 hrs by ADP-Glo assay | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2024) 67: 14702-14722 [PMID:39143914] |
| ChEMBL | Inhibition Assay: A partial protein of only a kinase domain of FLT3 protein was purchased from Carna Biosciences Inc., Japan, and tests were conducted as in Test Example 5. Test Example 5: A partial protein of only a kinase domain of RET protein was purchased from Carna Biosciences Inc., Japan. The phosphorylation activity toward a peptide substrate was investigated using an EZ reader (Caliper). Test compounds were each mixed with a protein solution to give 8 final concentrations from 100 nM to 0.03 nM, followed by addition of a mixed liquid of ATP and substrate peptide (Caliper) and reaction for 30 minutes. The ATP concentration used was 100 µM. A reaction liquid which contained protein but no test compound (in which the solvent DMSO alone was added at 0.8% in place of the test compound) was prepared, followed by reaction in the same manner with or without ATP addition. | B | 9.39 | pIC50 | 0.41 | nM | IC50 | US-8969336-B2. Diamino heterocyclic carboxamide compound (2015) |
| ChEMBL | Inhibition Assay: A partial protein of only a kinase domain of FLT3 protein was purchased from Carna Biosciences Inc., Japan, and tests were conducted as in Test Example 5. Test Example 5: A partial protein of only a kinase domain of RET protein was purchased from Carna Biosciences Inc., Japan. The phosphorylation activity toward a peptide substrate was investigated using an EZ reader (Caliper). Test compounds were each mixed with a protein solution to give 8 final concentrations from 100 nM to 0.03 nM, followed by addition of a mixed liquid of ATP and substrate peptide (Caliper) and reaction for 30 minutes. The ATP concentration used was 100 µM. A reaction liquid which contained protein but no test compound (in which the solvent DMSO alone was added at 0.8% in place of the test compound) was prepared, followed by reaction in the same manner with or without ATP addition. | B | 9.39 | pIC50 | 0.41 | nM | IC50 | US-8969336-B2. Diamino heterocyclic carboxamide compound (2015) |
| GtoPdb | - | - | 9.52 | pIC50 | ~0.3 | nM | IC50 | Blood (2017) 129: 257-260 [PMID:27908881] |
| ChEMBL | Inhibition of FLT3 (unknown origin) | B | 9.54 | pIC50 | 0.29 | nM | IC50 | RSC Med Chem (2022) 13: 798-816 [PMID:35923716] |
| ChEMBL | Inhibition of Flt3 (unknown origin) | B | 9.54 | pIC50 | 0.29 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| ChEMBL | Inhibition of N-terminal GST-tagged human FLT3 (564 to 993 residues) cytoplasmic domain expressed in baculovirus expression system by ELISA | B | 9.54 | pIC50 | 0.29 | nM | IC50 | Eur J Med Chem (2019) 178: 468-483 [PMID:31207462] |
| ChEMBL | Inhibition of FLT3 expressed in human SEMK2 cells assessed as reduction in FLT3 phosphorylation incubated for 1 hr by immunoblotting analysis | B | 9.54 | pIC50 | 0.29 | nM | IC50 | Eur J Med Chem (2020) 195: 112205-112205 [PMID:32272419] |
| ChEMBL | Inhibition of FLT3 (unknown origin) in presence of ATP | B | 9.54 | pIC50 | 0.29 | nM | IC50 | J Med Chem (2021) 64: 2878-2900 [PMID:33719439] |
| ChEMBL | Inhibition of FLT3 (unknown origin) | B | 9.54 | pIC50 | 0.29 | nM | IC50 | J Med Chem (2021) 64: 2878-2900 [PMID:33719439] |
| ChEMBL | Inhibition of wild type FLT3 (unknown origin) | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2020) 63: 12403-12428 [PMID:32659083] |
| ChEMBL | Inhibition of FLT3 ITD mutant (unknown origin) | B | 9.7 | pIC50 | 0.2 | nM | IC50 | RSC Med Chem (2023) 14: 1743-1754 [PMID:37731695] |
| ChEMBL | Inhibition of FLT3 D835Y mutant (unknown origin) | B | 9.73 | pIC50 | 0.19 | nM | IC50 | RSC Med Chem (2023) 14: 1743-1754 [PMID:37731695] |
| ChEMBL | Inhibition of FLT3 D835Y mutant (unknown origin) | B | 9.8 | pIC50 | 0.16 | nM | IC50 | J Med Chem (2020) 63: 12403-12428 [PMID:32659083] |
| 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] |
| 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] |
| 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 | 5.46 | pKd | 3438 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.57 | pKd | 2661 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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] |
| 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 | 5.77 | pKd | 1701 | 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 | 6.83 | pKd | 149 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.53 | pKd | 295 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 6.64 | pKd | 230 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.94 | pKd | 1143 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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 | 6.66 | pKd | 221 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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 | 6.61 | pKd | 247 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.55 | pKd | 2840 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| nemo like kinase/Serine/threonine-protein kinase NLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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] |
| 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] |
| 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] |
| 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 | 7.74 | pKd | 18 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| serine/threonine kinase 11/Serine/threonine-protein kinase STK11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5606] [GtoPdb: 2212] [UniProtKB: Q15831] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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] |
| 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] |
| 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 | 5.68 | pKd | 2092 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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 | 8.22 | pKd | 6 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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 | 7.17 | pKd | 68 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| transforming growth factor beta receptor 2/TGF-beta receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| 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 | 6.73 | pKd | 188 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| 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 | 5.8 | pKd | 1594 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| 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] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Inhibition of AXL (unknown origin) using poly (Glu, Tyr) as substrate after 60 mins by ELISA | B | 7.95 | pIC50 | 11.3 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 836-838 [PMID:30685094] |
| ChEMBL | LANCE Ultra TR-FRET Assay: The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different concentrations of pre-diluted compounds to a 384-well test plate and mixed for 10 minutes, in duplicate. The substrate and ATP were added to initiate the reaction, and incubated at room temperature for 90 minutes. The final reaction concentrations in the system were: 3 nM AXL, 4.75 uM ATP, 50 nM peptide, 50 mM Hepes pH7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Brij-35, and 2 mM DTT. The maximum concentration of the test compounds was 300 nM. After the reaction, the detection reagent containing 2 nM antibody and 10 mM EDTA was added and incubated at room temperature for 60 minutes. Finally, the enzyme activity in the presence of the compounds of the present disclosure at each concentration was measured by an Evnvision microplate reader, and the inhibition of the enzyme by the compounds at each concentration was calculated. The inhibitions of the enzyme activity by the compounds at different concentrations were then fitted using Graphpad 5.0 software according to the four-parameter equation, and the IC50 values were calculated. | B | 8.13 | pIC50 | 7.46 | nM | IC50 | US-11512074-B2. Substituted diamino heterocyclic carboxamide compound and a composition containing the compound and use thereof (2022) |
| ChEMBL | LANCE Ultra TR-FRET Assay: The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different concentrations of pre-diluted compounds to a 384-well test plate and mixed for 10 minutes, in duplicate. The substrate and ATP were added to initiate the reaction, and incubated at room temperature for 90 minutes. The final reaction concentrations in the system were: 3 nM AXL, 4.75 uM ATP, 50 nM peptide, 50 mM Hepes pH7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Brij-35, and 2 mM DTT. The maximum concentration of the test compounds was 300 nM. After the reaction, the detection reagent containing 2 nM antibody and 10 mM EDTA was added and incubated at room temperature for 60 minutes. Finally, the enzyme activity in the presence of the compounds of the present disclosure at each concentration was measured by an Evnvision microplate reader, and the inhibition of the enzyme by the compounds at each concentration was calculated. The inhibitions of the enzyme activity by the compounds at different concentrations were then fitted using Graphpad 5.0 software according to the four-parameter equation, and the IC50 values were calculated. | B | 8.13 | pIC50 | 7.35 | nM | IC50 | US-11512074-B2. Substituted diamino heterocyclic carboxamide compound and a composition containing the compound and use thereof (2022) |
| ChEMBL | LANCE Ultra TR-FRET Assay: The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different concentrations of pre-diluted compounds to a 384-well test plate and mixed for 10 minutes, in duplicate. The substrate and ATP were added to initiate the reaction, and incubated at room temperature for 90 minutes. The final reaction concentrations in the system were: 3 nM AXL, 4.75 uM ATP, 50 nM peptide, 50 mM Hepes pH7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Brij-35, and 2 mM DTT. The maximum concentration of the test compounds was 300 nM. After the reaction, the detection reagent containing 2 nM antibody and 10 mM EDTA was added and incubated at room temperature for 60 minutes. Finally, the enzyme activity in the presence of the compounds of the present disclosure at each concentration was measured by an Evnvision microplate reader, and the inhibition of the enzyme by the compounds at each concentration was calculated. The inhibitions of the enzyme activity by the compounds at different concentrations were then fitted using Graphpad 5.0 software according to the four-parameter equation, and the IC50 values were calculated. | B | 8.15 | pIC50 | 7.1 | nM | IC50 | US-11512074-B2. Substituted diamino heterocyclic carboxamide compound and a composition containing the compound and use thereof (2022) |
| ChEMBL | LANCE Ultra TR-FRET Assay: The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different concentrations of pre-diluted compounds to a 384-well test plate and mixed for 10 minutes, in duplicate. The substrate and ATP were added to initiate the reaction, and incubated at room temperature for 90 minutes. The final reaction concentrations in the system were: 3 nM AXL, 4.75 uM ATP, 50 nM peptide, 50 mM Hepes pH7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Brij-35, and 2 mM DTT. The maximum concentration of the test compounds was 300 nM. After the reaction, the detection reagent containing 2 nM antibody and 10 mM EDTA was added and incubated at room temperature for 60 minutes. Finally, the enzyme activity in the presence of the compounds of the present disclosure at each concentration was measured by an Evnvision microplate reader, and the inhibition of the enzyme by the compounds at each concentration was calculated. The inhibitions of the enzyme activity by the compounds at different concentrations were then fitted using Graphpad 5.0 software according to the four-parameter equation, and the IC50 values were calculated. | B | 8.15 | pIC50 | 7.01 | nM | IC50 | US-11512074-B2. Substituted diamino heterocyclic carboxamide compound and a composition containing the compound and use thereof (2022) |
| ChEMBL | LANCE Ultra TR-FRET Assay: The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different concentrations of pre-diluted compounds to a 384-well test plate and mixed for 10 minutes, in duplicate. The substrate and ATP were added to initiate the reaction, and incubated at room temperature for 90 minutes. The final reaction concentrations in the system were: 3 nM AXL, 4.75 uM ATP, 50 nM peptide, 50 mM Hepes pH7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Brij-35, and 2 mM DTT. The maximum concentration of the test compounds was 300 nM. After the reaction, the detection reagent containing 2 nM antibody and 10 mM EDTA was added and incubated at room temperature for 60 minutes. Finally, the enzyme activity in the presence of the compounds of the present disclosure at each concentration was measured by an Evnvision microplate reader, and the inhibition of the enzyme by the compounds at each concentration was calculated. The inhibitions of the enzyme activity by the compounds at different concentrations were then fitted using Graphpad 5.0 software according to the four-parameter equation, and the IC50 values were calculated. | B | 8.18 | pIC50 | 6.62 | nM | IC50 | US-11512074-B2. Substituted diamino heterocyclic carboxamide compound and a composition containing the compound and use thereof (2022) |
| ChEMBL | LANCE Ultra TR-FRET Assay: The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different concentrations of pre-diluted compounds to a 384-well test plate and mixed for 10 minutes, in duplicate. The substrate and ATP were added to initiate the reaction, and incubated at room temperature for 90 minutes. The final reaction concentrations in the system were: 3 nM AXL, 4.75 uM ATP, 50 nM peptide, 50 mM Hepes pH7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Brij-35, and 2 mM DTT. The maximum concentration of the test compounds was 300 nM. After the reaction, the detection reagent containing 2 nM antibody and 10 mM EDTA was added and incubated at room temperature for 60 minutes. Finally, the enzyme activity in the presence of the compounds of the present disclosure at each concentration was measured by an Evnvision microplate reader, and the inhibition of the enzyme by the compounds at each concentration was calculated. The inhibitions of the enzyme activity by the compounds at different concentrations were then fitted using Graphpad 5.0 software according to the four-parameter equation, and the IC50 values were calculated. | B | 8.19 | pIC50 | 6.5 | nM | IC50 | US-11512074-B2. Substituted diamino heterocyclic carboxamide compound and a composition containing the compound and use thereof (2022) |
| ChEMBL | LANCE Ultra TR-FRET Assay: The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different concentrations of pre-diluted compounds to a 384-well test plate and mixed for 10 minutes, in duplicate. The substrate and ATP were added to initiate the reaction, and incubated at room temperature for 90 minutes. The final reaction concentrations in the system were: 3 nM AXL, 4.75 uM ATP, 50 nM peptide, 50 mM Hepes pH7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Brij-35, and 2 mM DTT. The maximum concentration of the test compounds was 300 nM. After the reaction, the detection reagent containing 2 nM antibody and 10 mM EDTA was added and incubated at room temperature for 60 minutes. Finally, the enzyme activity in the presence of the compounds of the present disclosure at each concentration was measured by an Evnvision microplate reader, and the inhibition of the enzyme by the compounds at each concentration was calculated. The inhibitions of the enzyme activity by the compounds at different concentrations were then fitted using Graphpad 5.0 software according to the four-parameter equation, and the IC50 values were calculated. | B | 8.2 | pIC50 | 6.24 | nM | IC50 | US-11512074-B2. Substituted diamino heterocyclic carboxamide compound and a composition containing the compound and use thereof (2022) |
| ChEMBL | LANCE Ultra TR-FRET Assay: The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different concentrations of pre-diluted compounds to a 384-well test plate and mixed for 10 minutes, in duplicate. The substrate and ATP were added to initiate the reaction, and incubated at room temperature for 90 minutes. The final reaction concentrations in the system were: 3 nM AXL, 4.75 uM ATP, 50 nM peptide, 50 mM Hepes pH7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Brij-35, and 2 mM DTT. The maximum concentration of the test compounds was 300 nM. After the reaction, the detection reagent containing 2 nM antibody and 10 mM EDTA was added and incubated at room temperature for 60 minutes. Finally, the enzyme activity in the presence of the compounds of the present disclosure at each concentration was measured by an Evnvision microplate reader, and the inhibition of the enzyme by the compounds at each concentration was calculated. The inhibitions of the enzyme activity by the compounds at different concentrations were then fitted using Graphpad 5.0 software according to the four-parameter equation, and the IC50 values were calculated. | B | 8.23 | pIC50 | 5.87 | nM | IC50 | US-11512074-B2. Substituted diamino heterocyclic carboxamide compound and a composition containing the compound and use thereof (2022) |
| ChEMBL | LANCE Ultra TR-FRET Assay: The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different concentrations of pre-diluted compounds to a 384-well test plate and mixed for 10 minutes, in duplicate. The substrate and ATP were added to initiate the reaction, and incubated at room temperature for 90 minutes. The final reaction concentrations in the system were: 3 nM AXL, 4.75 uM ATP, 50 nM peptide, 50 mM Hepes pH7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Brij-35, and 2 mM DTT. The maximum concentration of the test compounds was 300 nM. After the reaction, the detection reagent containing 2 nM antibody and 10 mM EDTA was added and incubated at room temperature for 60 minutes. Finally, the enzyme activity in the presence of the compounds of the present disclosure at each concentration was measured by an Evnvision microplate reader, and the inhibition of the enzyme by the compounds at each concentration was calculated. The inhibitions of the enzyme activity by the compounds at different concentrations were then fitted using Graphpad 5.0 software according to the four-parameter equation, and the IC50 values were calculated. | B | 8.27 | pIC50 | 5.33 | nM | IC50 | US-11512074-B2. Substituted diamino heterocyclic carboxamide compound and a composition containing the compound and use thereof (2022) |
| ChEMBL | LANCE Ultra TR-FRET Assay: The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different concentrations of pre-diluted compounds to a 384-well test plate and mixed for 10 minutes, in duplicate. The substrate and ATP were added to initiate the reaction, and incubated at room temperature for 90 minutes. The final reaction concentrations in the system were: 3 nM AXL, 4.75 uM ATP, 50 nM peptide, 50 mM Hepes pH7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Brij-35, and 2 mM DTT. The maximum concentration of the test compounds was 300 nM. After the reaction, the detection reagent containing 2 nM antibody and 10 mM EDTA was added and incubated at room temperature for 60 minutes. Finally, the enzyme activity in the presence of the compounds of the present disclosure at each concentration was measured by an Evnvision microplate reader, and the inhibition of the enzyme by the compounds at each concentration was calculated. The inhibitions of the enzyme activity by the compounds at different concentrations were then fitted using Graphpad 5.0 software according to the four-parameter equation, and the IC50 values were calculated. | B | 8.29 | pIC50 | 5.15 | nM | IC50 | US-11512074-B2. Substituted diamino heterocyclic carboxamide compound and a composition containing the compound and use thereof (2022) |
| ChEMBL | Inhibition of AXL (unknown origin) using poly [Glu, Tyr] 4:1 as substrate incubated for 60 mins in presence of ATP by ELISA | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2021) 64: 3956-3975 [PMID:33733758] |
| ChEMBL | Inhibition of AXL (unknown origin) | B | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (2016) 59: 3593-3608 [PMID:26555154] |
| GtoPdb | - | - | 9.1 | pIC50 | ~0.8 | nM | IC50 | Blood (2017) 129: 257-260 [PMID:27908881] |
| ChEMBL | Inhibition of AXL (unknown origin) | B | 9.14 | pIC50 | 0.73 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| ChEMBL | Inhibition of AXL (unknown origin) | B | 9.14 | pIC50 | 0.73 | nM | IC50 | J Med Chem (2021) 64: 2878-2900 [PMID:33719439] |
| ChEMBL | Inhibition of AXL (unknown origin) in presence of ATP | B | 9.14 | pIC50 | 0.73 | nM | IC50 | J Med Chem (2021) 64: 2878-2900 [PMID:33719439] |
| ChEMBL | Inhibition of AXL (unknown origin) | B | 9.14 | pIC50 | 0.73 | nM | IC50 | Eur J Med Chem (2024) 272: 116475-116475 [PMID:38714043] |
| ChEMBL | Inhibition of N-terminal GST-tagged human AXL (464 to 885 residues) cytoplasmic domain expressed in baculovirus expression system by ELISA | B | 9.14 | pIC50 | 0.73 | nM | IC50 | Eur J Med Chem (2019) 178: 468-483 [PMID:31207462] |
| ChEMBL | Inhibition of AXL (unknown origin) | B | 9.14 | pIC50 | 0.73 | nM | IC50 | RSC Med Chem (2022) 13: 798-816 [PMID:35923716] |
| 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 | 5.39 | pKd | 4043 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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 | 6.35 | pKd | 445 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 5.86 | pKd | 1382 | 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 | 7.96 | pKd | 11 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MER proto-oncogene, tyrosine kinase in Human [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| GtoPdb | - | - | 8.52 | pIC50 | ~3 | nM | IC50 | Blood (2017) 129: 257-260 [PMID:27908881] |
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]