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 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]
