SB-431542 [Ligand Id: 8216] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL440084 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 3-phosphoinositide dependent protein kinase 1/3-phosphoinositide-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530] | ||||||||
| ChEMBL | Binding constant for full-length PDPK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase AMP-activated catalytic subunit alpha 1/5`-AMP-activated protein kinase catalytic subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131] | ||||||||
| ChEMBL | Binding constant for AMPK-alpha1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase AMP-activated catalytic subunit alpha 2/5`-AMP-activated protein kinase catalytic subunit alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2116] [GtoPdb: 1542] [UniProtKB: P54646] | ||||||||
| ChEMBL | Binding constant for AMPK-alpha2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912] | ||||||||
| ChEMBL | Binding constant for TNK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| activin A receptor type 1/Activin receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771] | ||||||||
| ChEMBL | Binding constant for ACVR1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| activin A receptor type 1B/Activin receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896] | ||||||||
| ChEMBL | Binding constant for ACVR1B kinase domain | B | 6.72 | pKd | 190 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| activin A receptor type IL/Activin receptor type-1-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5311] [GtoPdb: 1784] [UniProtKB: P37023] | ||||||||
| ChEMBL | Binding constant for ACVRL1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| activin A receptor type 2A/Activin receptor type-2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5616] [GtoPdb: 1791] [UniProtKB: P27037] | ||||||||
| ChEMBL | Binding constant for ACVR2A kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| activin A receptor type 2B/Activin receptor type-2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5466] [GtoPdb: 1792] [UniProtKB: Q13705] | ||||||||
| ChEMBL | Binding constant for ACVR2B kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
| ChEMBL | Binding constant for ALK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| TEK receptor tyrosine kinase/Angiopoietin-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| ChEMBL | Binding constant for TIE2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ankyrin repeat and kinase domain containing 1/Ankyrin repeat and protein kinase domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5547] [GtoPdb: 1932] [UniProtKB: Q8NFD2] | ||||||||
| ChEMBL | Binding constant for ANKK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| AP2 associated kinase 1/AP2-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3830] [GtoPdb: 1921] [UniProtKB: Q2M2I8] | ||||||||
| ChEMBL | Binding constant for AAK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| coenzyme Q8A/Atypical kinase COQ8A, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5550] [GtoPdb: 1927] [UniProtKB: Q8NI60] | ||||||||
| ChEMBL | Binding constant for ADCK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| coenzyme Q8B/Atypical kinase COQ8B, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5753] [GtoPdb: 1928] [UniProtKB: Q96D53] | ||||||||
| ChEMBL | Binding constant for full-length ADCK4 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Binding constant for AURKA kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| ChEMBL | Binding constant for AURKB kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| aurora kinase C/Aurora kinase C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9] | ||||||||
| ChEMBL | Binding constant for full-length AURKC | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| neurotrophic receptor tyrosine kinase 2/BDNF/NT-3 growth factors receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] | ||||||||
| ChEMBL | Binding constant for TRKB kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| BMP2 inducible kinase/BMP-2-inducible protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4522] [GtoPdb: 1941] [UniProtKB: Q9NSY1] | ||||||||
| ChEMBL | Binding constant for BIKE kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for BMPR1A kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for BMPR2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| calcium/calmodulin dependent protein kinase kinase 1/Calcium/calmodulin-dependent protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5256] [GtoPdb: 1956] [UniProtKB: Q8N5S9] | ||||||||
| ChEMBL | Binding constant for CAMKK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] | ||||||||
| ChEMBL | Binding constant for CAMKK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| calcium/calmodulin dependent protein kinase I/Calcium/calmodulin-dependent protein kinase type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2493] [GtoPdb: 1952] [UniProtKB: Q14012] | ||||||||
| ChEMBL | Binding constant for full-length CAMK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| calcium/calmodulin dependent protein kinase ID/Calcium/calmodulin-dependent protein kinase type 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5073] [GtoPdb: 1953] [UniProtKB: Q8IU85] | ||||||||
| ChEMBL | Binding constant for CAMK1D kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| calcium/calmodulin dependent protein kinase IG/Calcium/calmodulin-dependent protein kinase type 1G in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5258] [GtoPdb: 1954] [UniProtKB: Q96NX5] | ||||||||
| ChEMBL | Binding constant for CAMK1G kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| calcium/calmodulin-dependent protein kinase II alpha subunit/Calcium/calmodulin-dependent protein kinase type II subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7] | ||||||||
| ChEMBL | Binding constant for CAMK2A kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| calcium/calmodulin-dependent protein kinase II beta subunit/Calcium/calmodulin-dependent protein kinase type II subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554] | ||||||||
| ChEMBL | Binding constant for CAMK2B kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| calcium/calmodulin-dependent protein kinase II delta subunit/Calcium/calmodulin-dependent protein kinase type II subunit delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] | ||||||||
| ChEMBL | Binding constant for CAMK2D kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| calcium/calmodulin-dependent protein kinase II gamma subunit/Calcium/calmodulin-dependent protein kinase type II subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555] | ||||||||
| ChEMBL | Binding constant for CAMK2G kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| calcium/calmodulin dependent protein kinase IV/Calcium/calmodulin-dependent protein kinase type IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566] | ||||||||
| ChEMBL | Binding constant for CAMK4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| ChEMBL | Binding constant for PKAC-alpha kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase, cAMP-dependent, catalytic, beta subunit/cAMP-dependent protein kinase catalytic subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2918] [GtoPdb: 1477] [UniProtKB: P22694] | ||||||||
| ChEMBL | Binding constant for full-length PKAC-beta | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase X-linked/cAMP-dependent protein kinase catalytic subunit PRKX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5818] [GtoPdb: 2175] [UniProtKB: P51817] | ||||||||
| ChEMBL | Binding constant for full-length PRKX | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| casein kinase 1 alpha 1 like/Casein kinase I isoform alpha-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5520] [GtoPdb: 1996] [UniProtKB: Q8N752] | ||||||||
| ChEMBL | Binding constant for full-length CSNK1A1L | B | 5.23 | pKd | 5900 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] | ||||||||
| ChEMBL | Binding constant for full-length CSNK1D | B | 6.77 | pKd | 170 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | LanthaScreen Eu Kinase Binding Assay: Table 3: Small molecules were tested for their inhibitory activities towards casein kinase 1 delta (CK1δ) and 1 epsilon (CK1ϵ). The in vitro LanthaScreen Eu kinase binding assay was used to determine the IC50 values for 15 of the synthesized compounds and 5 commercial inhibitors including SB203580 (Table 3). Tested compounds displayed a wide range of affinity between 6.8 nM (high affinity=strong inhibition) to values over 1000 nM (low affinity=very weak inhibition). | B | 6.76 | pIC50 | 174 | nM | IC50 | US-10865384-B2. 2,4,5-tri-substituted azole-based casein kinase 1 inhibitors as inducers for cardiomyogenesis (2020) |
| casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
| ChEMBL | Binding constant for full-length CSNK1E | B | 6.59 | pKd | 260 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | LanthaScreen Eu Kinase Binding Assay: Table 3: Small molecules were tested for their inhibitory activities towards casein kinase 1 delta (CK1δ) and 1 epsilon (CK1ϵ). The in vitro LanthaScreen Eu kinase binding assay was used to determine the IC50 values for 15 of the synthesized compounds and 5 commercial inhibitors including SB203580 (Table 3). Tested compounds displayed a wide range of affinity between 6.8 nM (high affinity=strong inhibition) to values over 1000 nM (low affinity=very weak inhibition). | B | 6.83 | pIC50 | 147 | nM | IC50 | US-10865384-B2. 2,4,5-tri-substituted azole-based casein kinase 1 inhibitors as inducers for cardiomyogenesis (2020) |
| casein kinase 1 gamma 1/Casein kinase I isoform gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0] | ||||||||
| ChEMBL | Binding constant for CSNK1G1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| casein kinase 1 gamma 2/Casein kinase I isoform gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368] | ||||||||
| ChEMBL | Binding constant for full-length CSNK1G2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4] | ||||||||
| ChEMBL | Binding constant for full-length CSNK1G3 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400] | ||||||||
| ChEMBL | Binding constant for full-length CSNK2A1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| casein kinase 2, alpha prime polypeptide subunit/Casein kinase II subunit alpha` in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784] | ||||||||
| ChEMBL | Binding constant for full-length CSNK2A2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976] | ||||||||
| ChEMBL | Binding constant for PRKG1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Protein kinase G (PKG) 2/cGMP-dependent protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2896] [GtoPdb: 1493] [UniProtKB: Q13237] | ||||||||
| ChEMBL | Binding constant for PRKG2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578] | ||||||||
| ChEMBL | Binding constant for CIT kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 11A/Cyclin-dependent kinase 11A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5416] [GtoPdb: 1963] [UniProtKB: Q9UQ88] | ||||||||
| ChEMBL | Binding constant for CDC2L2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 11B/Cyclin-dependent kinase 11B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5808] [GtoPdb: 1964] [UniProtKB: P21127] | ||||||||
| ChEMBL | Binding constant for CDC2L1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 14/Cyclin-dependent kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6162] [GtoPdb: 1967] [UniProtKB: O94921] | ||||||||
| ChEMBL | Binding constant for full-length PFTK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 16/Cyclin-dependent kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4597] [GtoPdb: 1969] [UniProtKB: Q00536] | ||||||||
| ChEMBL | Binding constant for PCTK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 17/Cyclin-dependent kinase 17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5790] [GtoPdb: 1970] [UniProtKB: Q00537] | ||||||||
| ChEMBL | Binding constant for full-length PCTK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 18/Cyclin-dependent kinase 18 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5316] [GtoPdb: 1971] [UniProtKB: Q07002] | ||||||||
| ChEMBL | Binding constant for full-length PCTK3 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 19/Cyclin-dependent kinase 19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6002] [GtoPdb: 1972] [UniProtKB: Q9BWU1] | ||||||||
| ChEMBL | Binding constant for CDK11 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Binding constant for full-length CDK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 3/Cyclin-dependent kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4442] [GtoPdb: 1975] [UniProtKB: Q00526] | ||||||||
| ChEMBL | Binding constant for full-length CDK3 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Binding constant for full-length CDK5 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
| ChEMBL | Binding constant for full-length CDK7 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 8/Cyclin-dependent kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5719] [GtoPdb: 1980] [UniProtKB: P49336] | ||||||||
| ChEMBL | Binding constant for CDK8 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| ChEMBL | Binding constant for full-length CDK9 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| cyclin G associated kinase/Cyclin-G-associated kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4355] [GtoPdb: 2027] [UniProtKB: O14976] | ||||||||
| ChEMBL | Binding constant for GAK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| BMX non-receptor tyrosine kinase/Cytoplasmic tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813] | ||||||||
| ChEMBL | Binding constant for full-length BMX | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| death associated protein kinase 1/Death-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2558] [GtoPdb: 2002] [UniProtKB: P53355] | ||||||||
| ChEMBL | Binding constant for DAPK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| death associated protein kinase 2/Death-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3123] [GtoPdb: 2003] [UniProtKB: Q9UIK4] | ||||||||
| ChEMBL | Binding constant for full-length DAPK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| death associated protein kinase 3/Death-associated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2468] [GtoPdb: 2004] [UniProtKB: O43293] | ||||||||
| ChEMBL | Binding constant for full-length DLK | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for DAPK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832] | ||||||||
| ChEMBL | Binding constant for DDR2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for full-length MEK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for full-length MEK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for full-length MEK3 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase kinase 4/Dual specificity mitogen-activated protein kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2897] [GtoPdb: 2065] [UniProtKB: P45985] | ||||||||
| ChEMBL | Binding constant for MEK4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for MEK6 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759] | ||||||||
| ChEMBL | Binding constant for full-length CLK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] | ||||||||
| ChEMBL | Binding constant for CLK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761] | ||||||||
| ChEMBL | Binding constant for full-length CLK3 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1] | ||||||||
| ChEMBL | Binding constant for CLK4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
| ChEMBL | Binding constant for TTK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569] | ||||||||
| ChEMBL | Binding constant for TESK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463] | ||||||||
| ChEMBL | Binding constant for full-length DYRK1B | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| eukaryotic translation initiation factor 2 alpha kinase 4/eIF-2-alpha kinase GCN2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5358] [GtoPdb: 2018] [UniProtKB: Q9P2K8] | ||||||||
| ChEMBL | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709] | ||||||||
| ChEMBL | Binding constant for EPHA1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| ChEMBL | Binding constant for EPHA2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor A3/Ephrin type-A receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320] | ||||||||
| ChEMBL | Binding constant for EPHA3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764] | ||||||||
| ChEMBL | Binding constant for EPHA4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756] | ||||||||
| ChEMBL | Binding constant for EPHA5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor A6/Ephrin type-A receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4526] [GtoPdb: 1826] [UniProtKB: Q9UF33] | ||||||||
| ChEMBL | Binding constant for EPHA6 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] | ||||||||
| ChEMBL | Binding constant for EPHA7 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor A8/Ephrin type-A receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322] | ||||||||
| ChEMBL | Binding constant for EPHA8 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor B1/Ephrin type-B receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762] | ||||||||
| ChEMBL | Binding constant for EPHB1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] | ||||||||
| ChEMBL | Binding constant for EPHB2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753] | ||||||||
| ChEMBL | Binding constant for EPHB3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
| ChEMBL | Binding constant for EPHB4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Binding constant for EGFR kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for EGFR(E746-A750del) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for EGFR(G719C) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for EGFR(G719S) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for EGFR(L747-E749del, A750P) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for EGFR(L747-S752del, P753S) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for EGFR(L747-T751del,Sins) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for EGFR(L858R) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for EGFR(L861Q) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for EGFR(S752-I759del) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for DDR1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Binding constant for FGFR1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| ChEMBL | Binding constant for FGFR2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
| ChEMBL | Binding constant for FGFR3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for FGFR3(G697C) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
| ChEMBL | Binding constant for FGFR4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Binding constant for PTK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
| ChEMBL | Binding constant for full-length GSK3A | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Binding constant for full-length GSK3B | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Binding constant for MET kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Binding constant for TRKA kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa-B kinase subunit epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164] | ||||||||
| ChEMBL | Binding constant for full-length IKK-epsilon | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Binding constant for IGF1R kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Binding constant for INSR kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Insulin receptor-related receptor/Insulin receptor-related protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5483] [GtoPdb: 1802] [UniProtKB: P14616] | ||||||||
| ChEMBL | Binding constant for INSRR kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525] | ||||||||
| ChEMBL | Binding constant for PRKR kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for IRAK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376] | ||||||||
| ChEMBL | Binding constant for LTK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667] | ||||||||
| ChEMBL | Binding constant for full-length LIMK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| LIM domain kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5932] [GtoPdb: 2055] [UniProtKB: P53671] | ||||||||
| ChEMBL | Binding constant for full-length LIMK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| ChEMBL | Binding constant for CSF1R kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
| ChEMBL | Binding constant for MAPKAPK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] | ||||||||
| ChEMBL | Binding constant for MAPKAPK5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5] | ||||||||
| ChEMBL | Binding constant for full-length MKNK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] | ||||||||
| ChEMBL | Binding constant for MKNK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448] | ||||||||
| ChEMBL | Binding constant for full-length MARK3 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34] | ||||||||
| ChEMBL | Binding constant for MARK4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Binding constant for KIT kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for KIT(D816V) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for KIT(V559D,T670I) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for KIT(V559D,V654A) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for KIT(V559D) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding affinity to human KIT incubated for 1 hr by kinase binding assay | B | 5 | pKd | >10000 | nM | Kd | Eur J Med Chem (2011) 46: 2043-2057 [PMID:21429632] |
| ChEMBL | Binding affinity to human KIT D816V mutant incubated for 1 hr by kinase binding assay | B | 5 | pKd | >10000 | nM | Kd | Eur J Med Chem (2011) 46: 2043-2057 [PMID:21429632] |
| maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] | ||||||||
| ChEMBL | Binding constant for full-length MELK | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase, membrane associated tyrosine/threonine 1/Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640] | ||||||||
| ChEMBL | Binding constant for PKMYT1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Binding constant for full-length ERK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 10/Mitogen-activated protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779] | ||||||||
| ChEMBL | Binding constant for JNK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 11/Mitogen-activated protein kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759] | ||||||||
| ChEMBL | Binding constant for full-length p38-beta | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 12/Mitogen-activated protein kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778] | ||||||||
| ChEMBL | Binding constant for full-length p38-gamma | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Binding constant for full-length p38-alpha | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08] | ||||||||
| ChEMBL | Binding constant for ERK8 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Binding constant for full-length ERK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 4/Mitogen-activated protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5759] [GtoPdb: 2091] [UniProtKB: P31152] | ||||||||
| ChEMBL | Binding constant for ERK4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 6/Mitogen-activated protein kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5121] [GtoPdb: 2092] [UniProtKB: Q16659] | ||||||||
| ChEMBL | Binding constant for ERK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164] | ||||||||
| ChEMBL | Binding constant for ERK5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 8/Mitogen-activated protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983] | ||||||||
| ChEMBL | Binding constant for full-length JNK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase 9/Mitogen-activated protein kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984] | ||||||||
| ChEMBL | Binding constant for full-length JNK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase kinase kinase 10/Mitogen-activated protein kinase kinase kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2873] [GtoPdb: 2070] [UniProtKB: Q02779] | ||||||||
| ChEMBL | Binding constant for MLK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for MLK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mitogen-activated protein kinase kinase kinase 20 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2] | ||||||||
| ChEMBL | Binding constant for ZAK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for MAP3K4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for MAP3K5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192] | ||||||||
| ChEMBL | Binding constant for MLK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| mitogen-activated protein kinase kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5749] [GtoPdb: 2085] [UniProtKB: Q92918] | ||||||||
| ChEMBL | Binding constant for MAP4K1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for MAP4K3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for MAP4K4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for MAP4K5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| muscle associated receptor tyrosine kinase/Muscle, skeletal receptor tyrosine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5684] [GtoPdb: 1847] [UniProtKB: O15146] | ||||||||
| ChEMBL | Binding constant for MUSK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| myosin IIIA/Myosin-IIIa in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5546] [GtoPdb: 2112] [UniProtKB: Q8NEV4] | ||||||||
| ChEMBL | Binding constant for MYO3A kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| myosin IIIB/Myosin-IIIb in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5654] [GtoPdb: 2113] [UniProtKB: Q8WXR4] | ||||||||
| ChEMBL | Binding constant for MYO3B kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| myosin light chain kinase 2/Myosin light chain kinase 2, skeletal/cardiac muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2777] [GtoPdb: 1553] [UniProtKB: Q9H1R3] | ||||||||
| ChEMBL | Binding constant for MYLK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| myosin light chain kinase family member 4/Myosin light chain kinase family member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5426] [GtoPdb: 2111] [UniProtKB: Q86YV6] | ||||||||
| ChEMBL | Binding constant for SgK085 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Myosin light chain kinase, smooth muscle in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3062] [UniProtKB: P11799] | ||||||||
| ChEMBL | Binding constant for MLCK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746] | ||||||||
| ChEMBL | Binding constant for MYLK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| DM1 protein kinase/Myotonin-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5320] [GtoPdb: 1505] [UniProtKB: Q09013] | ||||||||
| ChEMBL | Binding constant for DMPK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470] | ||||||||
| ChEMBL | Binding constant for full-length TNK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Binding constant for TYK2(Kin.Dom.2/JH1 - catalytic) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288] | ||||||||
| ChEMBL | Binding constant for TRKC kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285] | ||||||||
| ChEMBL | Binding constant for ARK5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for SNARK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| ChEMBL | Binding constant for PIK3CA kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for PIK3CA(E545K) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| phosphatidylinositol-4-phosphate 5-kinase type 1 alpha/Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5969] [GtoPdb: 2164] [UniProtKB: Q99755] | ||||||||
| ChEMBL | Binding constant for full-length PIP5K1A | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| phosphatidylinositol-5-phosphate 4-kinase type 2 beta/Phosphatidylinositol 5-phosphate 4-kinase type-2 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5667] [GtoPdb: 2162] [UniProtKB: P78356] | ||||||||
| ChEMBL | Binding constant for full-length PIP5K2B | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735] | ||||||||
| ChEMBL | Binding constant for PHKG2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| phosphorylase kinase catalytic subunit gamma 1/Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4004] [GtoPdb: 2145] [UniProtKB: Q16816] | ||||||||
| ChEMBL | Binding constant for full-length PHKG1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] | ||||||||
| ChEMBL | Binding constant for PDGFRA kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| ChEMBL | Binding constant for PDGFRB kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase C delta/Protein kinase C delta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655] | ||||||||
| ChEMBL | Binding constant for PRKCD kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase C epsilon/Protein kinase C epsilon type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156] | ||||||||
| ChEMBL | Binding constant for PRKCE kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase C eta/Protein kinase C eta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723] | ||||||||
| ChEMBL | Binding constant for PRKCH kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase C theta/Protein kinase C theta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] | ||||||||
| ChEMBL | Binding constant for PRKCQ kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289] | ||||||||
| ChEMBL | Binding constant for full-length PTK2B | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882] | ||||||||
| ChEMBL | Binding constant for PTK6 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Binding constant for RET kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for RET(M918T) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922] | ||||||||
| ChEMBL | Binding constant for ROS1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Binding constant for SRC kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Binding constant for AKT1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| AKT serine/threonine kinase 2/RAC-beta serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751] | ||||||||
| ChEMBL | Binding constant for AKT2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| AKT serine/threonine kinase 3/RAC-gamma serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243] | ||||||||
| ChEMBL | Binding constant for AKT3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Raf-1 proto-oncogene, serine/threonine kinase/RAF proto-oncogene serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] | ||||||||
| ChEMBL | Binding constant for RAF1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546] | ||||||||
| ChEMBL | Binding constant for RIPK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| receptor interacting serine/threonine kinase 2/Receptor-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353] | ||||||||
| ChEMBL | Binding constant for RIPK2 kinase domain | B | 5.47 | pKd | 3400 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Binding constant for FLT3(ITD) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for FLT3(N841I) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for FLT3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for FLT3(D835H) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for FLT3(D835Y) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| erb-b2 receptor tyrosine kinase 2/Receptor tyrosine-protein kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Binding constant for ERBB2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Binding constant for RPS6KA1(Kin.Dom.1 - N-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for RPS6KA1(Kin.Dom.2 - C-terminal) kinase domain | B | 5.89 | pKd | 1300 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349] | ||||||||
| ChEMBL | Binding constant for RPS6KA2(Kin.Dom.1 - N-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for RPS6KA2(Kin.Dom.2 - C-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
| ChEMBL | Binding constant for RPS6KA3(Kin.Dom.1 - N-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676] | ||||||||
| ChEMBL | Binding constant for RPS6KA4(Kin.Dom.1 - C-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for RPS6KA4(Kin.Dom.2 - N-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582] | ||||||||
| ChEMBL | Binding constant for RPS6KA5(Kin.Dom.2 - N-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for RPS6KA5(Kin.Dom.1 - C-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32] | ||||||||
| ChEMBL | Binding constant for RPS6KA6(Kin.Dom.1 - C-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for RPS6KA6(Kin.Dom.2 - N-terminal) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804] | ||||||||
| ChEMBL | Binding constant for LOK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 16/Serine/threonine-protein kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3938] [GtoPdb: 2213] [UniProtKB: O75716] | ||||||||
| ChEMBL | Binding constant for STK16 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 17a/Serine/threonine-protein kinase 17A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4525] [GtoPdb: 2214] [UniProtKB: Q9UEE5] | ||||||||
| ChEMBL | Binding constant for DRAK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 17b/Serine/threonine-protein kinase 17B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3980] [GtoPdb: 2215] [UniProtKB: O94768] | ||||||||
| ChEMBL | Binding constant for full-length DRAK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0] | ||||||||
| ChEMBL | Binding constant for MST3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 25/Serine/threonine-protein kinase 25 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5552] [GtoPdb: 2218] [UniProtKB: O00506] | ||||||||
| ChEMBL | Binding constant for YSK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289] | ||||||||
| ChEMBL | Binding constant for full-length MST4 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188] | ||||||||
| ChEMBL | Binding constant for MST2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 32B/Serine/threonine-protein kinase 32B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5912] [GtoPdb: 1538] [UniProtKB: Q9NY57] | ||||||||
| ChEMBL | Binding constant for full-length YANK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 32C/Serine/threonine-protein kinase 32C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5405] [GtoPdb: 1539] [UniProtKB: Q86UX6] | ||||||||
| ChEMBL | Binding constant for YANK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 33/Serine/threonine-protein kinase 33 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6005] [GtoPdb: 2221] [UniProtKB: Q9BYT3] | ||||||||
| ChEMBL | Binding constant for full-length STK33 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 36/Serine/threonine-protein kinase 36 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4312] [GtoPdb: 2223] [UniProtKB: Q9NRP7] | ||||||||
| ChEMBL | Binding constant for STK36 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Serine/threonine kinase 38 like/Serine/threonine-protein kinase 38-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4851] [GtoPdb: 1518] [UniProtKB: Q9Y2H1] | ||||||||
| ChEMBL | Binding constant for NDR2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043] | ||||||||
| ChEMBL | Binding constant for full-length MST1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for BRAF kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for BRAF(V600E) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| BR serine/threonine kinase 1/Serine/threonine-protein kinase BRSK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5650] [GtoPdb: 1946] [UniProtKB: Q8TDC3] | ||||||||
| ChEMBL | Binding constant for BRSK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| BR serine/threonine kinase 2/Serine/threonine-protein kinase BRSK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3] | ||||||||
| ChEMBL | Binding constant for full-length BRSK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Binding constant for CHEK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase D1/Serine/threonine-protein kinase D1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139] | ||||||||
| ChEMBL | Binding constant for PRKD1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6] | ||||||||
| ChEMBL | Binding constant for PRKD2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase D3/Serine/threonine-protein kinase D3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806] | ||||||||
| ChEMBL | Binding constant for PRKD3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| doublecortin like kinase 1/Serine/threonine-protein kinase DCLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5683] [GtoPdb: 2005] [UniProtKB: O15075] | ||||||||
| ChEMBL | Binding constant for DCAMKL1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| doublecortin like kinase 2/Serine/threonine-protein kinase DCLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5519] [GtoPdb: 2006] [UniProtKB: Q8N568] | ||||||||
| ChEMBL | Binding constant for DCAMKL2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| doublecortin like kinase 3/Serine/threonine-protein kinase DCLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6123] [GtoPdb: 2007] [UniProtKB: Q9C098] | ||||||||
| ChEMBL | Binding constant for DCAMKL3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835] | ||||||||
| ChEMBL | Binding constant for LATS1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| large tumor suppressor kinase 2/Serine/threonine-protein kinase LATS2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5907] [GtoPdb: 1516] [UniProtKB: Q9NRM7] | ||||||||
| ChEMBL | Binding constant for LATS2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| microtubule affinity regulating kinase 1/Serine/threonine-protein kinase MARK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5940] [GtoPdb: 2097] [UniProtKB: Q9P0L2] | ||||||||
| ChEMBL | Binding constant for MARK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7] | ||||||||
| ChEMBL | Binding constant for MARK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25] | ||||||||
| ChEMBL | Binding constant for MRCKA kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| CDC42 binding protein kinase beta/Serine/threonine-protein kinase MRCK beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5052] [GtoPdb: 1508] [UniProtKB: Q9Y5S2] | ||||||||
| ChEMBL | Binding constant for MRCKB kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| CDC42 binding protein kinase gamma/Serine/threonine-protein kinase MRCK gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5615] [GtoPdb: 1506] [UniProtKB: Q6DT37] | ||||||||
| ChEMBL | Binding constant for DMPK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase N1/Serine/threonine-protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512] | ||||||||
| ChEMBL | Binding constant for PKN1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| protein kinase N2/Serine/threonine-protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] | ||||||||
| ChEMBL | Binding constant for PKN2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| NIMA related kinase 1/Serine/threonine-protein kinase Nek1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5855] [GtoPdb: 2114] [UniProtKB: Q96PY6] | ||||||||
| ChEMBL | Binding constant for NEK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| NIMA related kinase 2/Serine/threonine-protein kinase Nek2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3835] [GtoPdb: 2117] [UniProtKB: P51955] | ||||||||
| ChEMBL | Binding constant for NEK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| NIMA related kinase 5/Serine/threonine-protein kinase Nek5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5044] [GtoPdb: 2120] [UniProtKB: Q6P3R8] | ||||||||
| ChEMBL | Binding constant for NEK5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| NIMA related kinase 6/Serine/threonine-protein kinase Nek6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98] | ||||||||
| ChEMBL | Binding constant for NEK6 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| NIMA related kinase 7/Serine/threonine-protein kinase Nek7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4849] [GtoPdb: 2122] [UniProtKB: Q8TDX7] | ||||||||
| ChEMBL | Binding constant for full-length NEK7 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19] | ||||||||
| ChEMBL | Binding constant for NEK9 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| nemo like kinase/Serine/threonine-protein kinase NLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8] | ||||||||
| ChEMBL | Binding constant for full-length NLK | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4600] [GtoPdb: 2133] [UniProtKB: Q13153] | ||||||||
| ChEMBL | Binding constant for PAK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177] | ||||||||
| ChEMBL | Binding constant for PAK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| p21 (RAC1) activated kinase 3/Serine/threonine-protein kinase PAK 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2999] [GtoPdb: 2135] [UniProtKB: O75914] | ||||||||
| ChEMBL | Binding constant for full-length PAK3 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013] | ||||||||
| ChEMBL | Binding constant for PAK4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| p21 (RAC1) activated kinase 5/Serine/threonine-protein kinase PAK 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4524] [GtoPdb: 2138] [UniProtKB: Q9P286] | ||||||||
| ChEMBL | Binding constant for PAK7/PAK5 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5] | ||||||||
| ChEMBL | Binding constant for PAK6 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Binding constant for PIM1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| ChEMBL | Binding constant for PIM2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86] | ||||||||
| ChEMBL | Binding constant for PIM3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Binding constant for PLK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4] | ||||||||
| ChEMBL | Binding constant for PLK3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444] | ||||||||
| ChEMBL | Binding constant for PLK4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| RIO kinase 1/Serine/threonine-protein kinase RIO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5975] [GtoPdb: 2186] [UniProtKB: Q9BRS2] | ||||||||
| ChEMBL | Binding constant for full-length RIOK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| RIO kinase 3/Serine/threonine-protein kinase RIO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5659] [GtoPdb: 2188] [UniProtKB: O14730] | ||||||||
| ChEMBL | Binding constant for full-length RIOK3 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| salt inducible kinase 1/Serine/threonine-protein kinase SIK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6082] [GtoPdb: 2197] [UniProtKB: P57059] | ||||||||
| ChEMBL | Binding constant for SNF1LK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| salt inducible kinase 2/Serine/threonine-protein kinase SIK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5699] [GtoPdb: 2198] [UniProtKB: Q9H0K1] | ||||||||
| ChEMBL | Binding constant for full-length SNF1LK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| serine/threonine kinase 11/Serine/threonine-protein kinase STK11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5606] [GtoPdb: 2212] [UniProtKB: Q15831] | ||||||||
| ChEMBL | Binding constant for full-length LKB1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| TNNI3 interacting kinase/Serine/threonine-protein kinase TNNI3K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5260] [GtoPdb: 2247] [UniProtKB: Q59H18] | ||||||||
| ChEMBL | Binding constant for full-length TNNI3K | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| tousled like kinase 1/Serine/threonine-protein kinase tousled-like 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5388] [GtoPdb: 2242] [UniProtKB: Q9UKI8] | ||||||||
| ChEMBL | Binding constant for TLK1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| tousled like kinase 2/Serine/threonine-protein kinase tousled-like 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5404] [GtoPdb: 2243] [UniProtKB: Q86UE8] | ||||||||
| ChEMBL | Binding constant for TLK2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| SRSF protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4375] [GtoPdb: 2208] [UniProtKB: Q96SB4] | ||||||||
| ChEMBL | Binding constant for full-length SRPK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| SRSF protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5668] [GtoPdb: 2209] [UniProtKB: P78362] | ||||||||
| ChEMBL | Binding constant for full-length SRPK2 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| STE20 like kinase/STE20-like serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2] | ||||||||
| ChEMBL | Binding constant for SLK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| testis specific serine kinase 1B/Testis-specific serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6003] [GtoPdb: 2257] [UniProtKB: Q9BXA7] | ||||||||
| ChEMBL | Binding constant for full-length TSSK1 | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] | ||||||||
| ChEMBL | Binding constant for TGFBR1 kinase domain | B | 6.77 | pKd | 170 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Antagonistic activity at TGFBR1 | F | 1.03 | pKi | -1.03 | - | logKi | Bioorg Med Chem Lett (2010) 20: 1918-1923 [PMID:20176484] |
| ChEMBL | Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation counting | B | 7.77 | pKi | 17 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 326-329 [PMID:19914068] |
| ChEMBL | Inhibition of ALK5 in human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5 | pIC50 | 10000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of ALK5 in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5 | pIC50 | 10000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of ALK5 in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5 | pIC50 | 10000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of ALK5 in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5 | pIC50 | 10000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of ALK5 in Melphalan Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5 | pIC50 | 10000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of ALK5 in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 5 | pIC50 | 10000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of human recombinant ALK5 phosphorylation expressed in Sf9 cells | B | 5.81 | pIC50 | 1542 | nM | IC50 | J Med Chem (2007) 50: 3143-3147 [PMID:17552507] |
| ChEMBL | Inhibition of TGFbeta-induced downstream transcriptional activation of ALK5 (unknown origin) expressed in CHO-HIR cells assessed as intracellular translocation of EGFP-Smad2 after 2 hrs by luciferase assay | B | 6.46 | pIC50 | 350 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5850-5854 [PMID:24055046] |
| ChEMBL | Inhibition of TGFR-1 in human HepG2 cells expressing PAI-luciferase by luciferase reporter gene assay | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 326-329 [PMID:19914068] |
| ChEMBL | Inhibition of TGFbeta receptor | B | 6.9 | pIC50 | 125 | nM | IC50 | J Med Chem (2010) 53: 7287-7295 [PMID:20919678] |
| ChEMBL | Enzyme Activity Inhibition: 1. Preparation of a 1× kinase buffer: 40 mM Tris (pH 7.5), 20 mM MgCl2, 0.10% BSA, 1 mM DTT.2. Compound preparation: The final detection concentration of the compound was 10 μM, which was prepared to a 100-fold concentration, i.e., 1 mM. 100 μL of the 100-fold compound was added in the second well of the 384-well plate, and 60 μL of 100% DMSO was added to the other wells. 30 μL of compound from the second well was added to the third well, which was made a 3-fold dilution in sequence, diluting a total of 10 concentrations. 50 nL of the compound was transferred to the reaction plate with echo.3. Kinase reaction: The kinase was added to a 1× kinase buffer to form a 2× enzyme solution. The final concentration of the kinase solution was ALK5: 25 nM. The polypeptide TGFbR1 (purchased from Signal Chem, catalog number T36-58) and ATP were added to a 1× kinase buffer to form a 2× substrate solution. The final concentration of the substrate solution was peptide TGFbR1 0.1 mg/mL, ATP 7 μM. 2.5 μL of the 2× enzyme solution was added to the 384-well reaction plate (there was already 50 nL of 100% DMSO dissolved compound), and a 1× kinase buffer was added to a negative control well. The reaction solution was incubated at room temperature for 10 minutes. 2.5 μL of 2× substrate solution was added to the 384-well reaction plate. The 384-well plate was covered and incubated at 30° C. for 1 hour. ADP-Glo reagent (purchased from Promege, catalog number v9102) was equilibrated to room temperature. 5 μL of ADP-Glo reagent was transferred to the reaction well of the 384-well plate to stop the reaction.4. Detection of reaction results: 10 μL of kinase detection reagent was transferred to each well, shaken for 1 minute, and let stand at room temperature for 30 minutes. The sample luminescence value was read at Synegy. | B | 6.97 | pIC50 | 108 | nM | IC50 | US-11447490-B2. Aromatic heterocyclic substituted olefin compound, preparation method for same, pharmaceutical composition of same, and applications thereof (2022) |
| ChEMBL | Inhibitory Activity Toward ALK5 Enzyme: 1. Preparation of kinase buffer: 40 mM Tris (pH 7.5), 20 mM MgCl2, 0.10% BSA, 1 mM DTT.2. Preparation of the compound: the final concentration of the compound was 10 μM, and the compound was prepared to a 100-fold concentration, i.e, 1 mM. 100 μL compound of the 100-fold concentration was added to the second well of a 384-well plate, and 60 μL of 100% DMSO was added to other wells. 30 μL compound in the second well was transferred to the third well, and the compound was 3-fold diluted in sequence to give 10 different concentrations. 50 nL compound was transferred to a reaction plate by echo.3. Kinase reaction: the kinase was added to 1× kinase buffer to prepare 2× kinase solution. The final concentration of kinase solution was 25 nM of ALK5. Peptide TGFbR1 (purchased from Signal Chem, catalog number T36-58) and ATP were added to 1× kinase buffer to prepare 2× substrate solution. The final concentration of substrate solution was 0.1 mg/mL of polypeptide TGFbR1 and 7 μM of ATP. 2.5 μL of 2× kinase solution was added to a 384-well reaction plate (containing 50 nL compound dissolved in 100% DMSO), 1× kinase buffer was added to the negative control well. The reaction plated was incubated at room temperature for 10 minutes. 2.5 μL of 2× substrate solution was added to the 384-well reaction plate. The 384-well plate was covered with a lid and incubate at 30° C. for 1 hour. ADP-Glo reagent (purchased from Promege, catalog number v9102) was equilibrated to room temperature. 5 μL of ADP-Glo reagent was transferred to the reaction well of the 384-well plate to terminate the reaction.4. Determination of reaction results: 10 μL of kinase detection reagent was added to each reaction well, the 384-well plate was shaken for 1 minute, and allowed to stand for 30 minutes at room temperature. The luminescence value of the sample was read by Synegy.5. Curve Fitting: the data of the luminescence reading was copied from the Synegy program. | B | 6.97 | pIC50 | 108 | nM | IC50 | US-11466003-B2. Nitrogenous heterocyclic aromatic compound, preparation method therefor, pharmaceutical composition thereof, and application thereof (2022) |
| ChEMBL | Inhibition of TbetaR-1 (unknown origin) | B | 7.03 | pIC50 | 94 | nM | IC50 | Eur J Med Chem (2020) 191: 112154-112154 [PMID:32092587] |
| ChEMBL | Inhibition of ALK5 assessed as inhibition of immobilized Smad3 phosphorylation | B | 7.03 | pIC50 | 94 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4868-4872 [PMID:19616940] |
| ChEMBL | Inhibition of TGFR1 | B | 7.03 | pIC50 | 94 | nM | IC50 | Eur J Med Chem (2009) 44: 4259-4265 [PMID:19640613] |
| ChEMBL | Antagonistic activity at TGFBR1 | F | 7.03 | pIC50 | 94 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1918-1923 [PMID:20176484] |
| ChEMBL | Inhibition of Activin like receptor kinase 5, TGF beta type I receptor | B | 7.03 | pIC50 | 94 | nM | IC50 | J Med Chem (2002) 45: 999-1001 [PMID:11855979] |
| ChEMBL | Inhibition of N-terminal GST-tagged ALK5 (unknown origin) expressed in baculovirus expression system using GST-tagged Smad3 as substrate assessed as reduction in substrate phosphorylation | B | 7.03 | pIC50 | 94 | nM | IC50 | Eur J Med Chem (2024) 269: 116311-116311 [PMID:38508118] |
| GtoPdb | Inhibition of TGFBR1-induced Smad3 phosphorylation in vitro. | - | 7.03 | pIC50 | 94 | nM | IC50 | J Med Chem (2002) 45: 999-1001 [PMID:11855979] |
| ChEMBL | Inhibition of TGFbetaR1 (unknown origin) | B | 7.12 | pIC50 | 75 | nM | IC50 | Eur J Med Chem (2024) 271: 116395-116395 [PMID:38626523] |
| ChEMBL | Inhibition of TGFBR1 (unknown origin) | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged TGFbeta1 receptor (80 to end residues) expressed in baculovirus infected Sf9 insect cells using casein as substrate measured after 2 hrs by ADP-Glo assay | B | 7.17 | pIC50 | 67.1 | nM | IC50 | J Med Chem (2019) 62: 7961-7975 [PMID:31408333] |
| ChEMBL | Inhibition of TGFBR1 | B | 7.18 | pIC50 | 66 | nM | IC50 | J Med Chem (2012) 55: 9946-9957 [PMID:23130626] |
| ChEMBL | Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA | B | 6.76 | pEC50 | 172 | nM | EC50 | J Med Chem (2010) 53: 7287-7295 [PMID:20919678] |
| transforming growth factor beta receptor 2/TGF-beta receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173] | ||||||||
| ChEMBL | Binding constant for TGFBR2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay | B | 7.18 | pIC50 | 66 | nM | IC50 | J Med Chem (2012) 55: 9946-9957 [PMID:23130626] |
| TRAF2 and NCK interacting kinase/TRAF2 and NCK-interacting protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5] | ||||||||
| ChEMBL | Binding constant for TNIK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Binding constant for ABL1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for ABL1(H396P) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for ABL1(M351T) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for ABL1(Q252H) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for ABL1(T315I) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for ABL1(Y253F) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| ChEMBL | Binding constant for ABL1(E255K) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for ABL2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Blk in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451] | ||||||||
| ChEMBL | Binding constant for BLK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Binding constant for full-length BTK | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Binding constant for full-length CSK | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| FER tyrosine kinase/Tyrosine-protein kinase Fer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591] | ||||||||
| ChEMBL | Binding constant for FER kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Fes/Fps in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332] | ||||||||
| ChEMBL | Binding constant for FES kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fgr in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] | ||||||||
| ChEMBL | Binding constant for FGR kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685] | ||||||||
| ChEMBL | Binding constant for FRK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Binding constant for FYN kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] | ||||||||
| ChEMBL | Binding constant for HCK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881] | ||||||||
| ChEMBL | Binding constant for ITK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Binding constant for JAK1(Kin.Dom.1/JH2 - pseudokinase) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Binding constant for LCK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Binding constant for LYN kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| ChEMBL | Binding constant for MERTK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| tyrosine kinase with immunoglobulin like and EGF like domains 1/Tyrosine-protein kinase receptor Tie-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5274] [GtoPdb: 1841] [UniProtKB: P35590] | ||||||||
| ChEMBL | Binding constant for TIE1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| TYRO3 protein tyrosine kinase/Tyrosine-protein kinase receptor TYRO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5314] [GtoPdb: 1836] [UniProtKB: Q06418] | ||||||||
| ChEMBL | Binding constant for TYRO3 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Binding constant for AXL kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites/Tyrosine-protein kinase Srms in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5703] [GtoPdb: 2207] [UniProtKB: Q9H3Y6] | ||||||||
| ChEMBL | Binding constant for SRMS kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Binding constant for SYK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| tec protein tyrosine kinase/Tyrosine-protein kinase Tec in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680] | ||||||||
| ChEMBL | Binding constant for TEC kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681] | ||||||||
| ChEMBL | Binding constant for TXK kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| 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 | Binding constant for YES kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Binding constant for ZAP70 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] | ||||||||
| ChEMBL | Binding constant for FLT1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Binding constant for VEGFR2 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
| ChEMBL | Binding constant for FLT4 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
| WEE1 G2 checkpoint kinase/Wee1-like protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291] | ||||||||
| ChEMBL | Binding constant for WEE1 kinase domain | B | 5 | pKd | >10000 | nM | Kd | Nat Biotechnol (2008) 26: 127-132 [PMID:18183025] |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
