pamufetinib [Ligand Id: 10460] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3764045
  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
GtoPdb - - 7.41 pKi 39 nM Ki Mol Cancer Ther (2013) 12: 2685-96 [PMID:24140932]
ChEMBL Inhibition of recombinant N-terminal GST-tagged human Met using FLPeptide 2 as substrate after 90 mins by mobility shift assay B 7.49 pIC50 32 nM IC50 Eur J Med Chem (2016) 108: 495-504 [PMID:26717201]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
GtoPdb - - 7.92 pKi 12 nM Ki Mol Cancer Ther (2013) 12: 2685-96 [PMID:24140932]
ChEMBL Inhibition of recombinant N-terminal 6His-tagged VEGFR-2 (unknown origin) using FL-Peptide 22 as substrate after 90 mins by mobility shift assay B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2016) 108: 495-504 [PMID:26717201]

ChEMBL data shown on this page come from version 32:

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]