PIM447 [Ligand Id: 9790] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3651966 (Lgh-447, LGH-447, LGH447, NVP-LGH477, PIM 447, PIM-447, Pim kinase inhibitor lgh447) |
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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 | Affinity Phenotypic Cellular interaction: (Cell Titer-Gloxc2xae assay (proliferation in KMS11luc pS6RP cells, Promega)) EUB0001581a PIM1 | F | 6.74 | pIC50 | 180 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| 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) |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Cell Titer-Gloxc2xae assay (proliferation in KMS-11.luc cells, Promega)) EUB0001581a PIM1 | F | 6.77 | pEC50 | 170 | nM | EC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| 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 | Affinity Biochemical interaction: (AlphaScreen assay (500 uM ATP)) EUB0001581a PIM2 | B | 10.74 | pKi | 0.02 | nM | Ki | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Cell Titer-Gloxc2xae assay (proliferation in KMS11luc pS6RP cells, Promega)) EUB0001581a PIM2 | F | 6.74 | pIC50 | 180 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| 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] |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Cell Titer-Gloxc2xae assay (proliferation in KMS-11.luc cells, Promega)) EUB0001581a PIM2 | F | 6.77 | pEC50 | 170 | nM | EC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| 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 | Affinity Phenotypic Cellular interaction: (Cell Titer-Gloxc2xae assay (proliferation in KMS11luc pS6RP cells, Promega)) EUB0001581a PIM3 | F | 6.74 | pIC50 | 180 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| 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 | Affinity Phenotypic Cellular interaction: (Cell Titer-Gloxc2xae assay (proliferation in KMS-11.luc cells, Promega)) EUB0001581a PIM3 | F | 6.77 | pEC50 | 170 | nM | EC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| 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 34:
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]
