PIM447 [Ligand Id: 9790] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3651966 |
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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 | Inhibition of PDK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
| ChEMBL | Inhibition of ALK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| calcium/calmodulin-dependent protein kinase II beta subunit/CaM kinase II beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554] | ||||||||
| ChEMBL | Inhibition of CAMK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| casein kinase 1 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] | ||||||||
| ChEMBL | Inhibition of CK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| cyclin dependent kinase 2/CDK2/Cyclin A1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038470] [GtoPdb: 1973] [UniProtKB: P24941, P78396] | ||||||||
| ChEMBL | Inhibition of CDK2/Cyclin A (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| mitogen-activated protein kinase 9/c-Jun N-terminal kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984] | ||||||||
| ChEMBL | Inhibition of JNK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779] | ||||||||
| ChEMBL | Inhibition of JNK3 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| COUP-TF1/COUP transcription factor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1961789] [GtoPdb: 617] [UniProtKB: P10589] | ||||||||
| ChEMBL | Inhibition of COT1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
| ChEMBL | Inhibition of CDK1/cyclin B (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] | ||||||||
| ChEMBL | Inhibition of CDK4/cyclin D1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764] | ||||||||
| ChEMBL | Inhibition of EPHA4 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
| ChEMBL | Inhibition of EPHB4 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of HER1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Inhibition of FGFR1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| ChEMBL | Inhibition of FGFR2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
| ChEMBL | Inhibition of FGFR3 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ChEMBL | Inhibition of FGFR3 K650E mutant (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
| ChEMBL | Inhibition of FGFR4 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Inhibition of FAK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of GSK3beta (unknown origin) | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Inhibition of c-MET (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by patch clamp assay | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Inhibition of IGF1R (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of INS1R (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3] | ||||||||
| ChEMBL | Inhibition of IRAK4 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912] | ||||||||
| ChEMBL | Inhibition of RON (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
| ChEMBL | Inhibition of MK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] | ||||||||
| ChEMBL | Inhibition of MK5 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Inhibition of ERK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5] | ||||||||
| ChEMBL | Inhibition of MNK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibition of P38alpha (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| mitogen-activated protein kinase 12/MAP kinase p38 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778] | ||||||||
| ChEMBL | Inhibition of p38gamma (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] | ||||||||
| ChEMBL | Inhibition of MNK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9] | ||||||||
| ChEMBL | Inhibition of VPS34 (unknown origin) | B | 5.04 | pIC50 | >9100 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| ChEMBL | Inhibition of PI3Kalpha (unknown origin) | B | 5.04 | pIC50 | >9100 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
| ChEMBL | Inhibition of PI3Kbeta (unknown origin) | B | 5.04 | pIC50 | >9100 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] | ||||||||
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) | B | 5.04 | pIC50 | >9100 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) | B | 5.04 | pIC50 | >9100 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8] | ||||||||
| ChEMBL | Inhibition of PI4Kbeta (unknown origin) | B | 5.04 | pIC50 | >9100 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| 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 | Inhibition of PDGFRalpha (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Inhibition of PKCalpha (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| protein kinase C theta/Protein kinase C theta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] | ||||||||
| ChEMBL | Inhibition of PKCtheta (unknown origin) | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| protein kinase N1/Protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512] | ||||||||
| ChEMBL | Inhibition of PKN1 (unknown origin) | B | 5.31 | pIC50 | 4900 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| protein kinase N2/Protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] | ||||||||
| ChEMBL | Inhibition of PKN2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Inhibition of HER2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303] | ||||||||
| ChEMBL | Inhibition of HER4 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116] | ||||||||
| ChEMBL | Inhibition of ROCK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Inhibition of PKBalpha (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Inhibition of Aurora A (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
| ChEMBL | Inhibition of mTOR (unknown origin) | B | 5.04 | pIC50 | >9100 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177] | ||||||||
| ChEMBL | Inhibition of PAK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Inhibition of PIM1 kinase (unknown origin) using NH2-AGAGRSRHSSYPAGT-OH as substrate by kinase-Glo assay | B | 9 | pKi | <1 | nM | Ki | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ChEMBL | Inhibition of PIM1 (unknown origin) using Bad peptide NH2-AGAGRSRHSSYPAGT-OH as substrate measured after 10 mins in presence of ATP by luciferase-luciferin based Kinase-Glo luminescence assay | B | 9 | pKi | <1 | nM | Ki | J Med Chem (2020) 63: 14885-14904 [PMID:33258605] |
| GtoPdb | - | - | 11.22 | pKi | 0.01 | nM | Ki | J Med Chem (2015) 58: 8373-86 [PMID:26505898] |
| ChEMBL | ATP Depletion Assay: The activity of PIM1, PIM2, and PIM3 is measured using a luciferase-luciferin based ATP detection reagent to quantify ATP depletion resulting from kinase-catalyzed phosphoryl transfer to a peptide substrate. | B | 9 | pIC50 | 1 | nM | IC50 | US-8592455-B2. Kinase inhibitors and methods of their use (2013) |
| Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| ChEMBL | Inhibition of PIM2 kinase (unknown origin) using NH2-AGAGRSRHSSYPAGT-OH as substrate by kinase-Glo assay | B | 8.52 | pKi | <3 | nM | Ki | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ChEMBL | Inhibition of PIM2 (unknown origin) using Bad peptide NH2-AGAGRSRHSSYPAGT-OH as substrate measured after 10 mins in presence of ATP by luciferase-luciferin based Kinase-Glo luminescence assay | B | 8.52 | pKi | <3 | nM | Ki | J Med Chem (2020) 63: 14885-14904 [PMID:33258605] |
| GtoPdb | - | - | 10.74 | pKi | 0.02 | nM | Ki | J Med Chem (2015) 58: 8373-86 [PMID:26505898] |
| ChEMBL | Inhibition of PIM2 kinase (unknown origin) using Biotin-AGAGRSRHSSYPAGT-OH as substrate after 2 hrs by alphascreen assay | B | 10.74 | pKi | 0.02 | nM | Ki | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ChEMBL | ATP Depletion Assay: The activity of PIM1, PIM2, and PIM3 is measured using a luciferase-luciferin based ATP detection reagent to quantify ATP depletion resulting from kinase-catalyzed phosphoryl transfer to a peptide substrate. | B | 8.7 | pIC50 | 2 | nM | IC50 | US-8592455-B2. Kinase inhibitors and methods of their use (2013) |
| ChEMBL | Inhibition of PIM2 (unknown origin) | B | 10.74 | pIC50 | 0.02 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
| Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86] | ||||||||
| ChEMBL | Inhibition of PIM3 kinase (unknown origin) using NH2-AGAGRSRHSSYPAGT-OH as substrate by kinase-Glo assay | B | 8.52 | pKi | <3 | nM | Ki | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ChEMBL | Inhibition of PIM3 (unknown origin) using Bad peptide NH2-AGAGRSRHSSYPAGT-OH as substrate measured after 10 mins in presence of ATP by luciferase-luciferin based Kinase-Glo luminescence assay | B | 8.52 | pKi | <3 | nM | Ki | J Med Chem (2020) 63: 14885-14904 [PMID:33258605] |
| GtoPdb | - | - | 11.05 | pKi | 0.01 | nM | Ki | J Med Chem (2015) 58: 8373-86 [PMID:26505898] |
| ChEMBL | ATP Depletion Assay: The activity of PIM1, PIM2, and PIM3 is measured using a luciferase-luciferin based ATP detection reagent to quantify ATP depletion resulting from kinase-catalyzed phosphoryl transfer to a peptide substrate. | B | 8.7 | pIC50 | 2 | nM | IC50 | US-8592455-B2. Kinase inhibitors and methods of their use (2013) |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Inhibition of PLK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| WNK lysine deficient protein kinase 1/Serine/threonine-protein kinase WNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075173] [GtoPdb: 2280] [UniProtKB: Q9H4A3] | ||||||||
| ChEMBL | Inhibition of WNK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Inhibition of c-Kit (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Inhibition of cABL (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Inhibition of BTK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Inhibition of CSK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Inhibition of FYN (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] | ||||||||
| ChEMBL | Inhibition of HCK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Inhibition of JAK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Inhibition of JAK3 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Inhibition of LCK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Inhibition of LYN (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Inhibition of FLT3 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Inhibition of RET (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Inhibition of c-Src (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Inhibition of SYK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Inhibition of TYK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| 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 | Inhibition of YES (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| 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 | Inhibition of ZAP70 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition of KDR (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
