tafetinib [Ligand Id: 9921] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2180602 (SIM 010603, SIM-010603, Tafetinib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| GtoPdb | In a radiometric biochemical protein kinase assay. | - | 7.85 | pIC50 | 14 | nM | IC50 | Cancer Chemother Pharmacol (2012) 69: 173-83 [PMID:21638122] |
| ChEMBL | Inhibition of PDGFR-beta (unknown origin) | B | 8 | pIC50 | 10.1 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5630-5633 [PMID:23999040] |
| 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 | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2012) 55: 10797-10822 [PMID:23098265] |
| ChEMBL | Inhibition of c-KIT (unknown origin) | B | 8.62 | pIC50 | 2.4 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5630-5633 [PMID:23999040] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| GtoPdb | In a radiometric biochemical protein kinase assay. | - | 7.68 | pIC50 | 20.8 | nM | IC50 | Cancer Chemother Pharmacol (2012) 69: 173-83 [PMID:21638122] |
| ChEMBL | Inhibition of FLT3 | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2012) 55: 10797-10822 [PMID:23098265] |
| ChEMBL | Inhibition of FLT-3 (unknown origin) | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5630-5633 [PMID:23999040] |
| ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| GtoPdb | In a radiometric biochemical protein kinase assay. | - | 7.17 | pIC50 | 68.1 | nM | IC50 | Cancer Chemother Pharmacol (2012) 69: 173-83 [PMID:21638122] |
| ChEMBL | Inhibition of RET | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2012) 55: 10797-10822 [PMID:23098265] |
| ChEMBL | Inhibition of RET (unknown origin) | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5630-5633 [PMID:23999040] |
| 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 | Inhibition of VEGFR1 (unknown origin) | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5630-5633 [PMID:23999040] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| GtoPdb | In a radiometric biochemical protein kinase assay. | - | 8.3 | pIC50 | 5 | nM | IC50 | Cancer Chemother Pharmacol (2012) 69: 173-83 [PMID:21638122] |
| ChEMBL | Inhibition of VEGFR2 | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2012) 55: 10797-10822 [PMID:23098265] |
| ChEMBL | Inhibition of VEGFR2 (unknown origin) | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5630-5633 [PMID:23999040] |
| fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
| GtoPdb | In a radiometric biochemical protein kinase assay. | - | 7.92 | pIC50 | 11.9 | nM | IC50 | Cancer Chemother Pharmacol (2012) 69: 173-83 [PMID:21638122] |
| ChEMBL | Inhibition of VEGFR3 (unknown origin) | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5630-5633 [PMID:23999040] |
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]
