ibrutinib [Ligand Id: 6912] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1873475 (CRA-032765, Ibrutinib, Imbruvica, PC-32765, PCI 32765, PCI-32765, PCI-32765-00) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 26S protease 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] |
| Actin-related protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6090] [UniProtKB: P61160] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Actin-related protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105857] [UniProtKB: P61158] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.52 | pKd | >30000 | 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] |
| AP2 associated kinase 1/Adaptor-associated kinase 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenine phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105819] [UniProtKB: P07741] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenosine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3589] [GtoPdb: 1231] [UniProtKB: P55263] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenylate kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4938] [UniProtKB: P54819] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Mitochondrial adenine nucleotide translocator 2/ADP/ATP translocase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3709670] [GtoPdb: 1063] [UniProtKB: P05141] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Mitochondrial adenine nucleotide translocator 3/ADP/ATP translocase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105854] [GtoPdb: 1064] [UniProtKB: P12236] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase AMP-activated catalytic subunit alpha 1/AMP-activated protein kinase, alpha-1 subunit 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/AMP-activated protein kinase, gamma-1 subunit 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/AMP-activated protein kinase, gamma-2 subunit 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] |
| ATP-dependent RNA helicase DDX1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010634] [UniProtKB: Q92499] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX3X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5553] [UniProtKB: O00571] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX42 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105782] [UniProtKB: Q86XP3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DHX30 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105814] [UniProtKB: Q7L2E3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | 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] |
| Brain glycogen phosphorylase 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] |
| BCR activator of RhoGEF and GTPase/Breakpoint cluster region protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5146] [GtoPdb: 2755] [UniProtKB: P11274] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.84 | pKd | 1459 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin dependent protein kinase IG/CaM kinase I gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5258] [GtoPdb: 1954] [UniProtKB: Q96NX5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the 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 II delta subunit/CaM kinase II delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin-dependent protein kinase II gamma subunit/CaM kinase II gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin dependent protein kinase IV/CaM kinase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin dependent protein kinase kinase 2/CaM-kinase kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit 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 beta-1 catalytic subunit 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, gamma catalytic subunit 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 delta/Casein kinase I 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 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 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 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 2, alpha prime polypeptide subunit/Casein kinase II alpha (prime) 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 | 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] |
| cell division cycle 7/Cell division cycle 7-related protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5443] [GtoPdb: 1960] [UniProtKB: O00311] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 beta 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] |
| coenzyme Q8A/Chaperone activity of bc1 complex-like, 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] |
| Choline-phosphate cytidylyltransferase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105855] [UniProtKB: P49585] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Chromodomain-helicase-DNA-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105742] [UniProtKB: Q14839] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 9/c-Jun N-terminal kinase 2 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 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 His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP | B | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2019) 62: 4606-4623 [PMID:30943029] |
| 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 | 4.52 | pKd | >30000 | 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] |
| Cytochrome c1, heme protein, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105975] [UniProtKB: P08574] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Deoxycytidine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2447] [UniProtKB: P27707] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 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 II 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of MEK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| 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 | 6.61 | pKd | 243 | 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| 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] |
| dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the 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 1/Dual specificty 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] |
| Dynamin-like 120 kDa protein, 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] |
| Elongation factor Tu, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105970] [UniProtKB: P49411] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of recombinant human EPHA2 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 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 | 7.37 | pKd | 43 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 20 mins by HTRF assay | B | 6.41 | pIC50 | 390 | nM | IC50 | J Med Chem (2017) 60: 7725-7744 [PMID:28853575] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged wild-type EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay | B | 6.91 | pIC50 | 123 | nM | IC50 | Eur J Med Chem (2017) 131: 107-125 [PMID:28315597] |
| ChEMBL | Inhibition of human recombinant GST-tagged EGFR L858R mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 15 mins by HTRF assay | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2017) 60: 7725-7744 [PMID:28853575] |
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 7.02 | pIC50 | 96 | nM | IC50 | Bioorg Med Chem Lett (2021) 34: 127757-127757 [PMID:33359446] |
| ChEMBL | Inhibition of EGFR T790M mutant (unknown origin) | B | 7.29 | pIC50 | 51 | nM | IC50 | Bioorg Med Chem Lett (2021) 34: 127757-127757 [PMID:33359446] |
| ChEMBL | Inhibition of EGF-induced EGFR phosphorylation in human A431 cells preincubated for 24 hrs followed by EGF stimulation and measured after 10 mins by HTRF based immunoassay | B | 7.35 | pIC50 | 45 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1467-1472 [PMID:31620235] |
| ChEMBL | Inhibition of EGFR L858R/T790M double mutant (unknown origin) by HTRF assay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2019) 62: 2843-2848 [PMID:30768270] |
| ChEMBL | Inhibition of HER1 (unknown origin) | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2019) 62: 3228-3250 [PMID:30893553] |
| ChEMBL | Inhibition of EGFR phosphorylation in human A549 cells incubated for 4 hrs by Western blot assay | B | 7.78 | pIC50 | 16.6 | nM | IC50 | J Med Chem (2022) 65: 2694-2709 [PMID:35099969] |
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 7.8 | pIC50 | 16 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1467-1472 [PMID:31620235] |
| ChEMBL | Inhibition of human recombinant EGFR using Ulight-CAGAGAIETDKEYYTVKD measured after 15 mins in the presence of ATP by LANCE method | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2019) 169: 121-143 [PMID:30875504] |
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem (2019) 27: 3390-3395 [PMID:31221612] |
| ChEMBL | Inhibition of ErbB1 relative to control | B | 8.25 | pIC50 | 5.6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6258-6263 [PMID:21958547] |
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 8.25 | pIC50 | 5.6 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4171-4175 [PMID:28734581] |
| ChEMBL | Inhibition of recombinant human EGFR using Ulight-CAGAGAIETDKEYYTVKD as substrate incubate for 15 mins by LANCE assay | B | 8.25 | pIC50 | 5.6 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| GtoPdb | - | - | 8.28 | pIC50 | 5.3 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | Inhibition of N-terminal DYKDDDD-tagged EGFR (669 to 1210 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2021) 64: 16242-16270 [PMID:34672559] |
| ChEMBL | Inhibition of wild type EGFR (unknown origin) by HTRF assay | B | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (2019) 62: 2843-2848 [PMID:30768270] |
| ChEMBL | Inhibition of GST-tagged human EGFR (668 to 1210 residues) expressed in baculovirus expression system using poly-Glu-Tyr (4:1) as substrate incubated for 1 hrs by ELISA | B | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2022) 65: 2694-2709 [PMID:35099969] |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| 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] |
| 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] |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| ChEMBL | Inhibition Assay: When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences, Inc.) was used as a substrate. The purified recombinant human FGFR2 protein used in the test was purchased from Carna Biosciences, Inc. In the measurement of the inhibitory effect of the compounds, first, a test compound was gradually diluted with dimethylsulfoxide (DMSO) to a concentration that was 20 times higher than the final concentration. Next, the purified human FGFR2 protein, FL-Peptide 22 (final concentration: 1.5 .mu.M), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 75 .mu.M), and the test compound DMSO solution (final concentration of DMSO: 5%) were added to a reaction buffer (15 mM Tris-HCl pH 7.5, 0.01% Tween-20, 2 mM DTT), and the mixture was incubated at 25.degree. C. for 120 minutes to perform a kinase reaction. EDTA (final concentration: 30 mM) diluted with a separation buffer. | B | 6.55 | pIC50 | 280 | nM | IC50 | US-9108973-B2. 3,5-disubstituted alkynylbenzene compound and salt thereof (2015) |
| 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 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] |
| beta adrenergic receptor kinase 1/G-protein coupled receptor kinase 2 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] |
| G protein-coupled receptor kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6144] [GtoPdb: 1470] [UniProtKB: P43250] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the 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 | 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] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Binding affinity to human ERG | B | 5.96 | pKi | 1100 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 2939-2944 [PMID:30122225] |
| ChEMBL | Inhibition of human ERG expressed in CHO cells at holding potential of -80 mV by patch clamp method | B | 5.11 | pIC50 | 7700 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1863-1868 [PMID:33062165] |
| ChEMBL | Inhibition of human ERG | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3307-3311 [PMID:30243592] |
| inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit 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 | 4.52 | pKd | >30000 | 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 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] |
| 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.68 | pKd | 21089 | 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] |
| Liver glycogen phosphorylase 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] |
| colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| ChEMBL | Inhibition of recombinant human FMS using Ulight-TK peptide as substrate incubate for 15 mins by LANCE assay | B | 5.26 | pIC50 | 5545 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | Inhibition of recombinant human CSF1R using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 3/MAP kinase-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the 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] |
| mitogen-activated protein kinase 3/MAP kinase ERK1 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 1/MAP kinase ERK2 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 14/MAP kinase p38 alpha 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 11/MAP kinase p38 beta 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] |
| microtubule affinity regulating kinase 2/MAP/microtubule affinity-regulating kinase 2 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] |
| 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] |
| 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] |
| misshapen like kinase 1/Misshapen-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the 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 | 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 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 | 4.52 | pKd | >30000 | 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 | 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mixed lineage kinase 7 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 | 5.77 | pKd | 1705 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Multifunctional protein ADE2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5922] [UniProtKB: P22234] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Myosin-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105746] [UniProtKB: P35580] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Myosin-14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105888] [UniProtKB: Q7Z406] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| myosin 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 | 4.52 | pKd | >30000 | 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] |
| neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A 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] |
| tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| Neuron-derived orphan receptor 1/Nuclear receptor subfamily 4 group A member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1961792] [GtoPdb: 631] [UniProtKB: Q92570] | ||||||||
| ChEMBL | Inhibition of Tec (unknown origin) | B | 7.11 | pIC50 | 78 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| Nucleolar GTP-binding protein 1 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] |
| Nucleoside diphosphate kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2160] [UniProtKB: P22392] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Obg-like ATPase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105704] [UniProtKB: Q9NTK5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| PAS domain containing serine/threonine kinase/PAS domain-containing serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6054] [GtoPdb: 2139] [UniProtKB: Q96RG2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Peroxisomal acyl-coenzyme A oxidase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105817] [UniProtKB: O15254] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Phenylalanine--tRNA ligase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105969] [UniProtKB: Q9NSD9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Phosphatidylethanolamine-binding protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105856] [UniProtKB: P30086] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| phosphatidylinositol-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] |
| 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] |
| phosphorylase kinase catalytic subunit gamma 2/Phosphorylase kinase gamma subunit 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of recombinant human PDGFR-beta using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| Platelet glycoprotein VI (GPVI) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308912] [UniProtKB: Q9HCN6] | ||||||||
| ChEMBL | Inhibition of GP6 in human whole blood assessed as protein-mediated platelet aggregation preincubated for 15 mins followed by collagen stimulation and measured for 10 mins by multiple electrode aggregometry | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2020) 63: 12213-12242 [PMID:32463237] |
| 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 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C beta/Protein kinase C beta 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 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 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 kinase D3/Protein kinase C nu 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] |
| protein kinase C theta/Protein kinase C theta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase N1/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/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] |
| protein tyrosine kinase 2 beta/Protein tyrosine kinase 2 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the 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] |
| Putative nucleoside diphosphate kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105936] [UniProtKB: O60361] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the 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] |
| Quinone reductase 2 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Rab-like protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105853] [UniProtKB: Q5HYI8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 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 | 7.07 | pKd | 85 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Binding affinity to DNA-tagged recombinant ERBB2 (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | B | 8.92 | pKd | 1.2 | nM | Kd | J Med Chem (2020) 63: 5102-5118 [PMID:32083858] |
| ChEMBL | Inhibition of human recombinant HER2 using biotinyl-beta amyloid beta amyloid beta AAEEEEYFELVAKKK measured after 10 mins in the presence of ATP by HTRF assay | B | 7.66 | pIC50 | 22 | nM | IC50 | Eur J Med Chem (2019) 169: 121-143 [PMID:30875504] |
| ChEMBL | Inhibition of Her2 (unknown origin) | B | 8.03 | pIC50 | 9.4 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4171-4175 [PMID:28734581] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.03 | pIC50 | 9.4 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | Inhibition of human ErbB2 using using poly (4:1 Glu, Tyr) as substrate measured after 1 hr in presence of [gamma-33P]ATP | B | 8.03 | pIC50 | 9.4 | nM | IC50 | Medchemcomm (2018) 9: 697-704 [PMID:30108960] |
| ChEMBL | Inhibition of ErBB2 (unknown origin) | B | 8.03 | pIC50 | 9.4 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| GtoPdb | - | - | 8.19 | pIC50 | 6.4 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | Inhibition of His-tagged human recombinant ERBB2 (676 to 1255 residues) expressed in baculovirus expression system using Tyr 06 as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | B | 8.19 | pIC50 | 6.4 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127261-127261 [PMID:32527559] |
| ChEMBL | Inhibition of recombinant human ErbB2 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303] | ||||||||
| ChEMBL | Binding affinity to DNA-tagged recombinant ERBB4 (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | B | 8.62 | pKd | 2.4 | nM | Kd | J Med Chem (2020) 63: 5102-5118 [PMID:32083858] |
| ChEMBL | Inhibition of HER4 (unknown origin) | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2019) 62: 3228-3250 [PMID:30893553] |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.03 | pIC50 | 9.4 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | Inhibition of ERBB4 (unknown origin) | B | 8.15 | pIC50 | 7 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1467-1472 [PMID:31620235] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ERBB4 catalytic domain (708 to 993 residues) expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127261-127261 [PMID:32527559] |
| GtoPdb | - | - | 8.47 | pIC50 | 3.4 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | Inhibition of recombinant human ErbB4 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| ChEMBL | Inhibition of HER4 (unknown origin) | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Eur J Med Chem (2019) 169: 121-143 [PMID:30875504] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 10 | pIC50 | 0.1 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 10 | pIC50 | 0.1 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| Redox-regulatory protein FAM213A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879824] [UniProtKB: Q9BRX8] | ||||||||
| ChEMBL | Inhibition of PF-06658607 binding to recombinant C-terminal FLAG-tagged FAM213A (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay | B | 6.05 | pIC50 | 900 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| 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 B1/Ribosomal protein S6 kinase 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] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of RSK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| RNA cytidine acetyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105935] [UniProtKB: Q9H0A0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| S-adenosylmethionine synthase isoform type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3313835] [UniProtKB: P31153] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Septin-9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105891] [UniProtKB: Q9UHD8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 11/Serine/threonine-protein kinase 11 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] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| STE20 like kinase/Serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT 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/Serine/threonine-protein kinase AKT2 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/Serine/threonine-protein kinase AKT3 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] |
| 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] |
| aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| aurora kinase B/Serine/threonine-protein kinase Aurora-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] |
| 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] |
| microtubule affinity regulating kinase 3/Serine/threonine-protein kinase c-TAK1 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] |
| 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] |
| 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] |
| cyclin G associated kinase/Serine/threonine-protein kinase GAK 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 | 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] |
| integrin linked kinase/Serine/threonine-protein kinase ILK-1 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] |
| 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 | 5.72 | pKd | 1884 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK-A 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] |
| CDC42 binding protein kinase gamma/Serine/threonine-protein kinase MRCK gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5615] [GtoPdb: 1506] [UniProtKB: Q6DT37] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 4/Serine/threonine-protein kinase MST1 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] |
| serine/threonine kinase 3/Serine/threonine-protein kinase MST2 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-protein kinase MST4/Serine/threonine-protein kinase MST4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 7/Serine/threonine-protein kinase NEK7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4849] [GtoPdb: 2122] [UniProtKB: Q8TDX7] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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] |
| p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the 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/Serine/threonine-protein kinase PCTAIRE-1 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/Serine/threonine-protein kinase PCTAIRE-2 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] |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 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 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase X-linked/Serine/threonine-protein kinase PRKX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5818] [GtoPdb: 2175] [UniProtKB: P51817] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the 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/Serine/threonine-protein kinase RIPK2 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 | 7.24 | pKd | 57 | 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] |
| 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 | 4.52 | pKd | >30000 | 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| WEE1 G2 checkpoint kinase/Serine/threonine-protein kinase WEE1 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] |
| 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 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 I 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 II 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] |
| TP53 regulating kinase/TP53-regulating kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938223] [GtoPdb: 2248] [UniProtKB: Q96S44] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TRAF2 and NCK interacting kinase/TRAF2- and NCK-interacting 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] |
| protein kinase, membrane associated tyrosine/threonine 1/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] |
| tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL 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 | 5.77 | pKd | 1694 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.06 | pIC50 | 86.1 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.06 | pIC50 | 86.1 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| 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 | 6.04 | pKd | 919 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase BLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451] | ||||||||
| ChEMBL | Inhibition of BLK (unknown origin) by ADP-Glo assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Eur J Med Chem (2020) 199: 112339-112339 [PMID:32402933] |
| GtoPdb | - | - | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2012) 55: 4539-50 [PMID:22394077] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | Inhibition of BLK | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2012) 55: 4539-4550 [PMID:22394077] |
| ChEMBL | Inhibition of BLK (unknown origin) | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | Inhibition of recombinant human BLK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| GtoPdb | - | - | 10 | pIC50 | 0.1 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | Inhibition of recombinant full length human His-tagged BLK cytoplasmic domain expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | B | 10 | pIC50 | 0.1 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127261-127261 [PMID:32527559] |
| BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813] | ||||||||
| ChEMBL | Binding affinity to DNA-tagged recombinant BMX (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | B | 8.8 | pKd | 1.6 | nM | Kd | J Med Chem (2020) 63: 5102-5118 [PMID:32083858] |
| ChEMBL | Inhibition of full length recombinant human N-terminal GST-tagged BMX expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2017) 131: 107-125 [PMID:28315597] |
| ChEMBL | Inhibition of recombinant human BMX using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 8.24 | pIC50 | 5.8 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| ChEMBL | Inhibition of BMX (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1467-1472 [PMID:31620235] |
| ChEMBL | Inhibition of BMX (unknown origin) | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4171-4175 [PMID:28734581] |
| ChEMBL | Inhibition of BMX (unknown origin) | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | Inhibition of His-tagged recombinant full length human His-tagged BMX cytoplasmic domain expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127261-127261 [PMID:32527559] |
| ChEMBL | Inhibition of BMX | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2012) 55: 4539-4550 [PMID:22394077] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.1 | pIC50 | 0.8 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.1 | pIC50 | 0.8 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| GtoPdb | - | - | 9.1 | pIC50 | 0.8 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| GtoPdb | - | - | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2012) 55: 4539-50 [PMID:22394077] |
| ChEMBL | Inhibition of full-length N-terminal GST-tagged BMX (1 to 675 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2021) 64: 16242-16270 [PMID:34672559] |
| protein tyrosine kinase 6/Tyrosine-protein kinase BRK 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 | 7.51 | pKd | 31 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.48 | pIC50 | 3.3 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.48 | pIC50 | 3.3 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| 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 | 8 | pKd | 10 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Binding affinity to DNA-tagged recombinant BTK (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | B | 8.72 | pKd | 1.9 | nM | Kd | J Med Chem (2020) 63: 5102-5118 [PMID:32083858] |
| ChEMBL | Inhibition of His-tagged BTK (unknown origin) after 1.5 hrs by HTRF analysis | B | 6.37 | pKi | 425 | nM | Ki | J Med Chem (2019) 62: 3228-3250 [PMID:30893553] |
| ChEMBL | Reversible inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 2 to 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay | B | 8.32 | pKi | 4.8 | nM | Ki | Eur J Med Chem (2017) 131: 107-125 [PMID:28315597] |
| ChEMBL | Inhibition of BTK in human TMD8 cells assessed as reduction in cell proliferation incubated for 24 hrs by CCK-8 assay | B | 4.99 | pIC50 | 10350 | nM | IC50 | Eur J Med Chem (2020) 199: 112339-112339 [PMID:32402933] |
| ChEMBL | Inhibition of BTK C481S (unknown origin) | B | 6 | pIC50 | 1002 | nM | IC50 | J Med Chem (2020) 63: 10726-10741 [PMID:32432477] |
| ChEMBL | Inhibition of BTK C481S mutant (unknown origin) | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126877-126877 [PMID:31879210] |
| ChEMBL | Inhibition of BTK (unknown origin) by caliper mobility shift assay | B | 6.09 | pIC50 | 810 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | Inhibition of BTK in human basophils assessed as reduction in anti-IgE mouse IgG1 antibody Le2-stimulated CD63 expression on basophil preincubated for 30 mins in presence of IgE antibody B11 followed by anti-IgE mouse IgG1 antibody Le2 stimulation and measured after 15 mins by flow cytometry | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2020) 63: 5102-5118 [PMID:32083858] |
| ChEMBL | Inhibition of BTK in human whole blood cells after 30 mins by ELISA | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2019) 62: 3228-3250 [PMID:30893553] |
| ChEMBL | Inhibition of BTK in human whole blood derived-basophils assessed as suppression of IgE mediated-FcepsilonR ligation-stimulated CD63 expression | B | 6.77 | pIC50 | 171 | nM | IC50 | J Med Chem (2018) 61: 2227-2245 [PMID:29457982] |
| ChEMBL | Inhibition of BTK in human whole blood cells after 1 hr by ELISA | B | 6.98 | pIC50 | 105 | nM | IC50 | J Med Chem (2019) 62: 3228-3250 [PMID:30893553] |
| ChEMBL | Inhibition of BTK in human whole blood assessed as reduction in polyclonal anti-IgM antibody/human IL4-stimulated CD69 cell surface expression on B cells incubated for 16 hrs by FACS analysis | B | 7.18 | pIC50 | 66 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1467-1472 [PMID:31620235] |
| ChEMBL | Inhibition of BTK in human B cells assessed as reduction in anti-IgM/IL4-stimulated CD69 expression on B cells preincubated for 60 mins followed by anti-IgM antibody/IL4 stimulation and measured after 16 hrs by flow cytometry | B | 7.18 | pIC50 | 66 | nM | IC50 | J Med Chem (2020) 63: 5102-5118 [PMID:32083858] |
| ChEMBL | Inhibition of BTK in human whole blood cells after 120 mins by ELISA | B | 7.24 | pIC50 | 57.5 | nM | IC50 | J Med Chem (2019) 62: 3228-3250 [PMID:30893553] |
| ChEMBL | Inhibition of human recombinant full length N-terminal His tagged BTK C481S mutant expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay | B | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2019) 178: 767-781 [PMID:31234030] |
| ChEMBL | Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by HTRF assay | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2020) 63: 5102-5118 [PMID:32083858] |
| ChEMBL | Inhibition of recombinant full-length N-terminal His-tagged human BTK C481S mutant expressed in baculovirus infected Sf9 insect cells using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 7.84 | pIC50 | 14.4 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| ChEMBL | Inhibition of BTK in human whole blood | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3419-3424 [PMID:30290988] |
| ChEMBL | Inhibition of BTK in human WBC | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3307-3311 [PMID:30243592] |
| ChEMBL | Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2014) 57: 5112-5128 [PMID:24915291] |
| ChEMBL | Inhibition of BTK in whole blood (unknown origin) | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2939-2944 [PMID:30122225] |
| ChEMBL | Inhibition of BTK in human Ramos B cells assessed as reduction in BCR-stimulated calcium flux after 1 hr in dark condition measured for 180 sec | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2019) 62: 3228-3250 [PMID:30893553] |
| ChEMBL | Inhibition of BTK C481S mutant (unknown origin) in presence of 1 mM ATP by microplate reader assay | B | 7.89 | pIC50 | 12.9 | nM | IC50 | J Med Chem (2021) 64: 14129-14141 [PMID:34529443] |
| ChEMBL | Inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2017) 131: 107-125 [PMID:28315597] |
| ChEMBL | Inhibition of BTK in human whole blood-derived CD19+ B cells assessed as suppression of anti-IgM stimulated-CD69 expression preincubated for 1 hr followed by IgM stimulation for 18 hrs by FACS analysis | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2018) 61: 2227-2245 [PMID:29457982] |
| ChEMBL | Inhibition of BTK in human whole blood assessed as activation of anti-IgM-induced CD69 expression by flow cytometry analysis | B | 8.09 | pIC50 | 8.14 | nM | IC50 | J Med Chem (2021) 64: 14129-14141 [PMID:34529443] |
| ChEMBL | Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis | B | 8.12 | pIC50 | >7.5 | nM | IC50 | J Med Chem (2014) 57: 5112-5128 [PMID:24915291] |
| ChEMBL | Inhibition of recombinant full-length human N-terminal GST-fused BTK (2 to 659 residues) expressed in baculovirus expression system using biotin-labelled peptide as substrate measured after 50 mins by TR-FRET assay | B | 8.26 | pIC50 | 5.49 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 225-229 [PMID:30522954] |
| ChEMBL | Inhibition of full length human N-terminal GST-tagged BTK (2 to 659 residues) expressed in baculovirus expression system using biotinylated substrate after 50 mins by HTRF assay | B | 8.26 | pIC50 | 5.49 | nM | IC50 | Bioorg Med Chem (2018) 26: 2165-2172 [PMID:29567295] |
| ChEMBL | Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by immunoblot analysis | B | 8.3 | pIC50 | <5 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1467-1472 [PMID:31620235] |
| ChEMBL | Inhibition of full length human unphosphorylated BTK using FITC-Ahx-TSELKKVVALYDYMPMNAND-NH2 as substrate incubated for 60 mins in presence of ATP at Km concentration | B | 8.3 | pIC50 | 5 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1467-1472 [PMID:31620235] |
| ChEMBL | Inhibition of BTK in goat anti-human IgM F(ab')2-stimulated human PBMC assessed as suppression of BCR-induced CD69 expression on B cells pretreated for 1 hr followed by blood stimulation measured after overnight incubation by flow cytometry | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3419-3424 [PMID:30290988] |
| ChEMBL | Inhibition of BTK in human PBMC assessed as reduction in anti-IgM-induced CD69 expression incubated for 1 hr by flow cytometric analysis | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2939-2944 [PMID:30122225] |
| ChEMBL | Inhibition of BTK in human PBMC | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3307-3311 [PMID:30243592] |
| ChEMBL | Inhibition of BTK (unknown origin) after 1 hr by TR-FRET assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2015) 23: 6250-6257 [PMID:26344595] |
| ChEMBL | Inhibition of human recombinant BTK incubated for 5 mins by HTRF kinase assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2015) 23: 6059-6068 [PMID:26277759] |
| ChEMBL | Inhibition of human recombinant full length BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay | B | 8.41 | pIC50 | 3.89 | nM | IC50 | Bioorg Med Chem (2019) 27: 4124-4142 [PMID:31395509] |
| ChEMBL | Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2019) 62: 7923-7940 [PMID:31381333] |
| ChEMBL | Inhibition of full-length human C-terminal His6-tagged BTK C481S mutant expressed in Sf9 insect cells using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | ACS Med Chem Lett (2019) 10: 80-85 [PMID:30655951] |
| ChEMBL | Inhibition of full-length human recombinant BTK using FITC-Ahx-TSELKKVVALYDYMPMNAND-NH2 as substrate measured after 60 mins by caliper assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Med Chem (2020) 63: 5102-5118 [PMID:32083858] |
| ChEMBL | Inhibition of wild type BTK (unknown origin) | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2020) 63: 10726-10741 [PMID:32432477] |
| ChEMBL | Inhibition of BTK (unknown origin) | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126877-126877 [PMID:31879210] |
| ChEMBL | Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus expression system using TK1 as substrate incubated for 60 mins by HTRF assay | B | 8.7 | pIC50 | 2 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1863-1868 [PMID:33062165] |
| ChEMBL | Inhibition of human recombinant full length N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Eur J Med Chem (2019) 178: 767-781 [PMID:31234030] |
| ChEMBL | Inhibition of BTK phosphorylation in human U-937 cells incubated for 4 hrs by Western blot assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2022) 65: 2694-2709 [PMID:35099969] |
| GtoPdb | - | - | 8.82 | pIC50 | 1.5 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | Inhibition of BTK (unknown origin) preincubated for 1 hr followed by ATP addition measured after 1 hr by immobilized metal ion affinity-based fluorescence polarization assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2017) 60: 8552-8564 [PMID:28945083] |
| ChEMBL | Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology. Measurements were performed in a reaction volume of 50 uL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 uM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25uL of 1x Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1x Lance buffer were added in a 25 uL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour. | B | 8.85 | pIC50 | 1.4 | nM | IC50 | US-9133201-B2. Inhibitors of Bruton's tyrosine kinase (2015) |
| ChEMBL | Inhibition of BTK (unknown origin) in the presence of ATP by caliper mobility shift assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | Eur J Med Chem (2019) 169: 121-143 [PMID:30875504] |
| ChEMBL | Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue incubated for 24 hrs by Western blot analysis | B | 8.96 | pIC50 | 1.09 | nM | IC50 | J Med Chem (2021) 64: 14129-14141 [PMID:34529443] |
| ChEMBL | Inhibition of recombinant full length human N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells using poly (4:1 Glu, Tyr) as substrate after 60 mins by ADP-Glo assay | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2018) 26: 4537-4543 [PMID:30077608] |
| ChEMBL | Inhibition of BTK (unknown origin) using poly(Glu, Tyr) 4:1 as substrate incubated in presence of [gamma33P]ATP by image analyser | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2020) 204: 112636-112636 [PMID:32731189] |
| ChEMBL | Inhibition of wild type BTK (unknown origin) in presence of 1 mM ATP by microplate reader assay | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2021) 64: 14129-14141 [PMID:34529443] |
| ChEMBL | Inhibition of BTK in human Ramos cells assessed as reduction of IgM stimulated PLCgamma2 (Y1217) phosphorylation after 24 hrs by western blot assay | B | 9 | pIC50 | 0.99 | nM | IC50 | J Med Chem (2021) 64: 14129-14141 [PMID:34529443] |
| ChEMBL | Inhibition of full-length N-terminal GST tagged BTK (2 to 659 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA | B | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2021) 64: 16242-16270 [PMID:34672559] |
| ChEMBL | Inhibition of BTK (unknown origin) by ADP-Glo assay | B | 9.05 | pIC50 | 0.89 | nM | IC50 | Eur J Med Chem (2020) 199: 112339-112339 [PMID:32402933] |
| ChEMBL | Inhibition of human BTK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2022) 65: 2694-2709 [PMID:35099969] |
| ChEMBL | Time-Resolved Fluorescence Resonance Energy Transfer Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology. | B | 9.14 | pIC50 | 0.72 | nM | IC50 | US-8497277-B2. Inhibitors of Bruton's tyrosine kinase (2013) |
| ChEMBL | Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology. Measurements were performed in a reaction volume of 50 uL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 uM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25uL of 1x Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1x Lance buffer were added in a 25 uL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour. | B | 9.14 | pIC50 | 0.72 | nM | IC50 | US-9133201-B2. Inhibitors of Bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro Inhibition Assay: Measurements were performed in a reaction volume of 50 μL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 μM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25 μL of 1× Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1× Lance buffer were added in a 25 μL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour. The TR-FRET signal was measured on a multimode plate reader with an excitation wavelength (πEx) of 330 nm and detection wavelengths (πEm) of 615 and 665 nm. Activity was determined by the ratio of the fluorescence at 665 nm to that at 615 nm. For each compound, enzyme activity was measured at various concentrations of compound. Negative control reactions were performed in the absence of inhibitor in replicates of six, and two no-enzyme controls were used to determine baseline fluorescence levels. | B | 9.14 | pIC50 | 0.72 | nM | IC50 | US-8476284-B2. Inhibitors of Bruton's tyrosine kinase (2013) |
| ChEMBL | Inhibition of BTK (unknown origin) | B | 9.14 | pIC50 | 0.72 | nM | IC50 | Bioorg Med Chem Lett (2021) 34: 127757-127757 [PMID:33359446] |
| ChEMBL | Inhibition of BTK (unknown origin) by ADP-gloassay | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Eur J Med Chem (2019) 164: 304-316 [PMID:30605829] |
| ChEMBL | Inhibition of BTK (unknown origin) assessed as reduction in phosphorylation of coumarin and fluorescein-labeled FRET peptide substrate incubated for 1 hr by Z-Lyte assay | B | 9.19 | pIC50 | 0.64 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3052-3059 [PMID:27210433] |
| ChEMBL | Inhibition of BTK (unknown origin) by ELISA | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem (2019) 27: 3390-3395 [PMID:31221612] |
| ChEMBL | Inhibition of recombinant human full-length N-terminal His6-tagged BTK expressed in baculovirus infected Sf21insect cells using poly (4:1 Glu, Tyr) as substrate measured after 1 hr by ELISA | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Medchemcomm (2018) 9: 697-704 [PMID:30108960] |
| ChEMBL | Inhibition of N-terminal DYKDDDDK tagged biotinylated activated human recombinant BTK using FITC-labeled Srctide peptide substrate by mobility shift assay | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (2018) 61: 8917-8933 [PMID:30216722] |
| GtoPdb | - | - | 9.3 | pIC50 | 0.5 | nM | IC50 | ChemMedChem (2007) 2: 58-61 [PMID:17154430] |
| ChEMBL | Inhibition of PF-06658607 binding to BTK in human Ramos cells after 1 hr by gel-based ABPP assay | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| ChEMBL | Inhibition of BTK (unknown origin) after 60 mins by FRET assay | B | 9.3 | pIC50 | <0.5 | nM | IC50 | J Med Chem (2020) 63: 441-469 [PMID:31550151] |
| ChEMBL | Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET Assay | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6258-6263 [PMID:21958547] |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology. Measurements were performed in a reaction volume of 50 uL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 uM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25uL of 1x Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1x Lance buffer were added in a 25 uL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour. | B | 9.3 | pIC50 | <0.5 | nM | IC50 | US-9133201-B2. Inhibitors of Bruton's tyrosine kinase (2015) |
| ChEMBL | Time-Resolved Fluorescence Resonance Energy Transfer Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology. | B | 9.3 | pIC50 | <0.5 | nM | IC50 | US-8497277-B2. Inhibitors of Bruton's tyrosine kinase (2013) |
| ChEMBL | Inhibition of BTK (unknown origin) One-hour enzymatic assay without pre-incubation | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2021) 38: 127862-127862 [PMID:33609659] |
| ChEMBL | Irreversible inhibition of recombinant BTK (unknown origin) incubated for 1 hr by FRET assay | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3052-3059 [PMID:27210433] |
| ChEMBL | Inhibition of human BTK by enzymatic assay | B | 9.3 | pIC50 | <=0.5 | nM | IC50 | J Med Chem (2012) 55: 4539-4550 [PMID:22394077] |
| ChEMBL | Inhibition of BTK (unknown origin) | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem (2015) 23: 6059-6068 [PMID:26277759] |
| ChEMBL | Inhibition of recombinant Btk after 60 mins | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2012) 55: 6243-6262 [PMID:22621397] |
| ChEMBL | Inhibition of BTK (unknown origin) | B | 9.3 | pIC50 | <0.5 | nM | IC50 | Eur J Med Chem (2017) 142: 493-505 [PMID:28986130] |
| ChEMBL | Inhibition of human BTK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method | B | 9.34 | pIC50 | 0.46 | nM | IC50 | J Med Chem (2019) 62: 7923-7940 [PMID:31381333] |
| ChEMBL | Inhibition of His-tagged recombinant human His-tagged full length BTK expressed in baculovirus expression system using Tyr01 peptide as substrate preincubated for 1 hr by Z'lyte assay | B | 9.37 | pIC50 | 0.43 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127261-127261 [PMID:32527559] |
| ChEMBL | Inhibition of full length recombinant human N-terminal His-tagged BTK expressed in baculovirus infected Sf9 cells using poly (4:1 Glu, Tyr) peptide as substrate after 60 mins by ADP-Glo assay | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem (2018) 26: 4179-4186 [PMID:30006143] |
| ChEMBL | Inhibition of recombinant human BTK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| ChEMBL | Inhibition of N-terminal His-tagged full length human recombinant BTK expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay | B | 9.47 | pIC50 | 0.34 | nM | IC50 | Eur J Med Chem (2017) 126: 444-455 [PMID:27912175] |
| ChEMBL | Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay | B | 9.47 | pIC50 | 0.34 | nM | IC50 | Bioorg Med Chem (2017) 25: 765-772 [PMID:27956037] |
| ChEMBL | Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells after 60 mins by ADP-Glo kinase assay | B | 9.47 | pIC50 | 0.34 | nM | IC50 | Eur J Med Chem (2017) 135: 60-69 [PMID:28432946] |
| ChEMBL | Inhibition of N-terminal DYKDDDDK tagged biotinylated unactivated human recombinant BTK using FITC-labeled Srctide peptide substrate by by mobility shift assay | B | 9.48 | pIC50 | 0.33 | nM | IC50 | J Med Chem (2018) 61: 8917-8933 [PMID:30216722] |
| ChEMBL | Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay | B | 9.52 | pIC50 | 0.3 | nM | IC50 | ACS Med Chem Lett (2016) 7: 1050-1055 [PMID:27994736] |
| ChEMBL | Inhibition of recombinant full-length N-terminal His-tagged human BTK expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Eur J Med Chem (2018) 143: 1847-1857 [PMID:29146136] |
| ChEMBL | Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem (2020) 28: 115236-115236 [PMID:31843459] |
| ChEMBL | Inhibition of BTK (unknown origin) | B | 9.68 | pIC50 | 0.21 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3736-3740 [PMID:30343954] |
| ChEMBL | Inhibition of recombinant human full length N-terminal GST-tagged BTK (2 to 659 residues) expressed in baculovirus expression system using FITC-AHA-EEPLYWSFPAKKK-NH2 substrate measured after 90 mins by off-chip mobility shift assay | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3419-3424 [PMID:30290988] |
| ChEMBL | Inhibition of human full length BTK using FITC-AHA-EEPLYWSFPAKKK-NH2 as substrate after 90 mins by microfluid mobility shift assay | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2939-2944 [PMID:30122225] |
| ChEMBL | Inhibition of human BTK using KVEKIGEGTYGVVYK as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition by filter binding method | B | 9.96 | pIC50 | 0.11 | nM | IC50 | J Med Chem (2017) 60: 8552-8564 [PMID:28945083] |
| ChEMBL | Inhibition of full-length human His-tagged BTK expressed in baculovirus expression system using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay | B | 10 | pIC50 | 0.1 | nM | IC50 | ACS Med Chem Lett (2019) 10: 80-85 [PMID:30655951] |
| ChEMBL | Inhibition of recombinant human BTK using fluoresceinated peptide as substrate after 60 mins fluorescence assay | B | 10.1 | pIC50 | 0.08 | nM | IC50 | J Med Chem (2019) 62: 3228-3250 [PMID:30893553] |
| 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 | 6.4 | pKd | 399 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of CSK (unknown origin) | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.66 | pIC50 | 2.2 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.66 | pIC50 | 2.2 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| FER tyrosine kinase/Tyrosine-protein kinase FER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 5.09 | pIC50 | 8070 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 5.09 | pIC50 | 8070 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase FES 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] |
| FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] | ||||||||
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.64 | pIC50 | 2.3 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.64 | pIC50 | 2.3 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | Inhibition of FGR (unknown origin) | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| 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 | 6.23 | pKd | 589 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of FRK (unknown origin) | B | 7.53 | pIC50 | 29.2 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| 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 | 6.52 | pKd | 305 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of recombinant human FYN using biotinyl-beta Abeta-Abeta AYQAEENTYDEYEN as substrate incubate for 60 mins by LANCE assay | B | 7.02 | pIC50 | 96 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.02 | pIC50 | 95.6 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.02 | pIC50 | 95.6 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| GtoPdb | - | - | 7.54 | pIC50 | 29 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| 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 | 7.38 | pKd | 42 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| GtoPdb | - | - | 7.54 | pIC50 | 29 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | Inhibition of HCK (unknown origin) | B | 7.82 | pIC50 | 15.3 | nM | IC50 | Bioorg Med Chem Lett (2021) 34: 127757-127757 [PMID:33359446] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.43 | pIC50 | 3.7 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.43 | pIC50 | 3.7 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | Inhibition of HCK (unknown origin) | B | 8.43 | pIC50 | 3.7 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881] | ||||||||
| ChEMBL | Binding affinity to DNA-tagged recombinant ITK (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | B | 7.24 | pKd | 57 | nM | Kd | J Med Chem (2020) 63: 5102-5118 [PMID:32083858] |
| ChEMBL | Inhibition of ITK phosphorylation in human Jurkat cells incubated for 4 hrs by Western blot assay | B | 6.75 | pIC50 | 178.5 | nM | IC50 | J Med Chem (2022) 65: 2694-2709 [PMID:35099969] |
| ChEMBL | Inhibition of recombinant full length human GST-tagged ITK expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | B | 6.77 | pIC50 | 168 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127261-127261 [PMID:32527559] |
| ChEMBL | Inhibition of ITK (unknown origin) by ADP-Glo assay | B | 7 | pIC50 | 99 | nM | IC50 | Eur J Med Chem (2020) 199: 112339-112339 [PMID:32402933] |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.93 | pIC50 | 11.7 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.93 | pIC50 | 11.7 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.93 | pIC50 | 11.7 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.93 | pIC50 | 11.7 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | Inhibition of ITK (unknown origin) | B | 7.97 | pIC50 | 10.7 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | Inhibition of human ITK using using myelin basic protein as substrate measured after 1 hr in presence of [gamma-33P]ATP | B | 7.97 | pIC50 | 10.7 | nM | IC50 | Medchemcomm (2018) 9: 697-704 [PMID:30108960] |
| ChEMBL | Inhibition of full-length N-terminal GST-tagged ITK (2 to 620 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2021) 64: 16242-16270 [PMID:34672559] |
| GtoPdb | - | - | 8.31 | pIC50 | 4.9 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | Inhibition of human ITK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2022) 65: 2694-2709 [PMID:35099969] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of JAK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged JAK1 (850 to 1154 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2020) 28: 115236-115236 [PMID:31843459] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate incubate for 60 mins by LANCE assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2020) 28: 115236-115236 [PMID:31843459] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Binding affinity to DNA-tagged recombinant JAK3 (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis | B | 7.43 | pKd | 37 | nM | Kd | J Med Chem (2020) 63: 5102-5118 [PMID:32083858] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay | B | 6.84 | pIC50 | 146 | nM | IC50 | Eur J Med Chem (2017) 131: 107-125 [PMID:28315597] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged JAK3 (781-end residues) expressed in baculovirus infected Sf9 cells using poly (4:1 Glu, Tyr) peptide as substrate after 60 mins by ADP-Glo assay | B | 7 | pIC50 | <100 | nM | IC50 | Bioorg Med Chem (2018) 26: 4179-4186 [PMID:30006143] |
| GtoPdb | - | - | 7.49 | pIC50 | 32 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | Inhibition of recombinant human GST-tagged JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using tyrosine-6 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127261-127261 [PMID:32527559] |
| ChEMBL | Inhibition of human recombinant JAK3 using Ulight-CAGAGAIETDKEYYTVKD measured after 60 mins in the presence of ATP by LANCE method | B | 7.66 | pIC50 | 22 | nM | IC50 | Eur J Med Chem (2019) 169: 121-143 [PMID:30875504] |
| ChEMBL | Inhibition of recombinant human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay | B | 7.69 | pIC50 | 20.3 | nM | IC50 | Bioorg Med Chem (2020) 28: 115236-115236 [PMID:31843459] |
| ChEMBL | Inhibition of recombinant N-terminal GST-tagged human JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay | B | 7.79 | pIC50 | 16.1 | nM | IC50 | Eur J Med Chem (2018) 143: 1847-1857 [PMID:29146136] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay | B | 7.79 | pIC50 | 16.1 | nM | IC50 | Bioorg Med Chem (2020) 28: 115254-115254 [PMID:31866272] |
| ChEMBL | Inhibition of recombinant human JAK3 using Ulight-CAGAGAIETDKEYYTVKD as substrate incubate for 60 mins by LANCE assay | B | 7.79 | pIC50 | 16.1 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.98 | pIC50 | 10.4 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.98 | pIC50 | 10.4 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.98 | pIC50 | 10.4 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.98 | pIC50 | 10.4 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| 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 | 6.99 | pKd | 103 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | In Vitro Inhibition Assay: Measurements were performed in a reaction volume of 50 μL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 μM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25 μL of 1× Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1× Lance buffer were added in a 25 μL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour. The TR-FRET signal was measured on a multimode plate reader with an excitation wavelength (πEx) of 330 nm and detection wavelengths (πEm) of 615 and 665 nm. Activity was determined by the ratio of the fluorescence at 665 nm to that at 615 nm. For each compound, enzyme activity was measured at various concentrations of compound. Negative control reactions were performed in the absence of inhibitor in replicates of six, and two no-enzyme controls were used to determine baseline fluorescence levels. | B | 7.01 | pKi | 97 | nM | Ki | US-8476284-B2. Inhibitors of Bruton's tyrosine kinase (2013) |
| ChEMBL | Inhibition of recombinant human LCK using Ulight-Poly GAT[EAY(1:1:1)]n as substrate incubate for 10 mins by LANCE assay | B | 7.48 | pIC50 | 33.2 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| GtoPdb | - | - | 8.2 | pIC50 | 6.3 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.7 | pIC50 | 2 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.7 | pIC50 | 2 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.7 | pIC50 | 2 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.7 | pIC50 | 2 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| 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 | 6.83 | pKd | 148 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | In Vitro Inhibition Assay: Measurements were performed in a reaction volume of 50 μL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 μM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25 μL of 1× Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1× Lance buffer were added in a 25 μL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour. The TR-FRET signal was measured on a multimode plate reader with an excitation wavelength (πEx) of 330 nm and detection wavelengths (πEm) of 615 and 665 nm. Activity was determined by the ratio of the fluorescence at 665 nm to that at 615 nm. For each compound, enzyme activity was measured at various concentrations of compound. Negative control reactions were performed in the absence of inhibitor in replicates of six, and two no-enzyme controls were used to determine baseline fluorescence levels. | B | 7.85 | pKi | 14 | nM | Ki | US-8476284-B2. Inhibitors of Bruton's tyrosine kinase (2013) |
| ChEMBL | Inhibition of LYN-A expressed in Sf9 cells after 60 mins by TR-FRET Assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6258-6263 [PMID:21958547] |
| ChEMBL | Inhibition of recombinant human LYN using biotinyl-beta Abeta-Abeta AKVEKIGEGTYGVVYK as substrate incubate for 120 mins by LANCE assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.79 | pIC50 | 16.2 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.79 | pIC50 | 16.2 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor 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 | 5.8 | pKd | 1578 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of recombinant human FLT3 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| ChEMBL | Inhibition of FLT3 (unknown origin) | B | 7.14 | pIC50 | 73 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ret 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 | 4.74 | pKd | 18050 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of RET | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2012) 55: 4539-4550 [PMID:22394077] |
| ChEMBL | Inhibition of RET (unknown origin) | B | 7.44 | pIC50 | 36.5 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | Inhibition of recombinant human RET using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 8.28 | pIC50 | 5.2 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| SRC proto-oncogene, non-receptor tyrosine kinase/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 | 7.01 | pKd | 97 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 6.58 | pIC50 | 262.6 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 6.58 | pIC50 | 262.6 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | Inhibition of recombinant human SRC using Ulight-Poly GAT[EAY(1:1:1)]n as substrate incubate for 10 mins by LANCE assay | B | 6.77 | pIC50 | 171 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| ChEMBL | Inhibition of SRC (unknown origin) | B | 6.92 | pIC50 | 119.2 | nM | IC50 | Bioorg Med Chem Lett (2021) 34: 127757-127757 [PMID:33359446] |
| ChEMBL | Inhibition of SRC (unknown origin) by ADP-Glo assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2020) 199: 112339-112339 [PMID:32402933] |
| GtoPdb | - | - | 7.72 | pIC50 | 19 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | Inhibition of SRC S345C mutant (unknown origin) | B | 7.8 | pIC50 | 15.88 | nM | IC50 | Bioorg Med Chem Lett (2021) 34: 127757-127757 [PMID:33359446] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 5 | pIC50 | >10000 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 5 | pIC50 | >10000 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | Inhibition of SYK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| 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 | 7.6 | pKd | 25 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.11 | pIC50 | 77.8 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 7.11 | pIC50 | 77.8 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| GtoPdb | - | - | 8.15 | pIC50 | 7 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| ChEMBL | Inhibition of His-tagged recombinant human TEC expressed in baculovirus expression system preincubated for 1 hr by Z'lyte assay | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127261-127261 [PMID:32527559] |
| TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681] | ||||||||
| ChEMBL | Inhibition of recombinant human TXK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2018) 61: 4608-4627 [PMID:29715023] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged TXK (260 to 527 residues) expressed in baculovirus expression system using tyrosine-6 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127261-127261 [PMID:32527559] |
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| tyrosine kinase 2/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] |
| 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 | 7.57 | pKd | 27 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.19 | pIC50 | 6.5 | nM | IC50 | US-9181263-B2. Inhibitors of bruton's tyrosine kinase (2015) |
| ChEMBL | In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate. | B | 8.19 | pIC50 | 6.5 | nM | IC50 | US-9278100-B2. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors (2016) |
| ChEMBL | Inhibition of recombinant human YES using biotinyl-beta Abeta-Abeta AYQAEENTYDEYEN as substrate incubate for 30 mins by LANCE assay | B | 8.19 | pIC50 | 6.5 | nM | IC50 | Eur J Med Chem (2018) 145: 96-112 [PMID:29324347] |
| GtoPdb | - | - | 8.39 | pIC50 | 4.1 | nM | IC50 | N Engl J Med (2016) 374: 323-32 [PMID:26641137] |
| Tyrosyl-tRNA synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3179] [UniProtKB: P54577] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| U5 small nuclear ribonucleoprotein 200 kDa helicase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105972] [UniProtKB: O75643] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| aarF domain containing kinase 1/Uncharacterized 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 | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Uncharacterized protein FLJ45252 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105933] [UniProtKB: Q6ZSR9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | 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] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
