CH7057288 [Ligand Id: 12237] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4457566 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 (2022) 65: 12427-12444 [PMID:36066182] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Inhibition of CDK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| 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 (2022) 65: 12427-12444 [PMID:36066182] |
| 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 MET (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of INSR (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Inhibition of TRKA G595R mutant (unknown origin) | B | 5.52 | pIC50 | 3000 | nM | IC50 | Eur J Med Chem (2022) 238: 114451-114451 [PMID:35617855] |
| ChEMBL | Inhibition of human TrkA G595R mutant expressed in mouse NIH/3T3 cells by HTRF assay | B | 7.08 | pIC50 | 83 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126624-126624 [PMID:31444087] |
| ChEMBL | Inhibition of human wild type TrkA kinase domain expressed in mouse NIH/3T3 cells by HTRF assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126624-126624 [PMID:31444087] |
| GtoPdb | - | - | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| ChEMBL | Inhibition of TRKA (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| ChEMBL | Inhibition of human TrkA G667C mutant expressed in mouse NIH/3T3 cells by HTRF assay | B | 9.17 | pIC50 | 0.68 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126624-126624 [PMID:31444087] |
| neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] | ||||||||
| ChEMBL | Inhibition of TRKB (unknown origin) | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288] | ||||||||
| GtoPdb | - | - | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| ChEMBL | Inhibition of TRKC (unknown origin) | B | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| 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 (2022) 65: 12427-12444 [PMID:36066182] |
| 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 (2022) 65: 12427-12444 [PMID:36066182] |
| 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 AKT1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Inhibition of CHK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] | ||||||||
| ChEMBL | Inhibition of RAF1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| 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 (2022) 65: 12427-12444 [PMID:36066182] |
| 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 | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| 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 Src (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
| 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 | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2022) 65: 12427-12444 [PMID:36066182] |
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]
