metatinib [Ligand Id: 12614] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2143592
  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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  • macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
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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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  • MER proto-oncogene, tyrosine kinase in Human [GtoPdb: 1837] [UniProtKB: Q12866]
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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]
ChEMBL Competitive inhibition of c-Met (unknown origin) in presence of ATP B 8.77 pIC50 1.7 nM IC50 Eur J Med Chem (2016) 108: 495-504 [PMID:26717201]
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 8.52 pIC50 <3 nM IC50 Eur J Med Chem (2016) 108: 495-504 [PMID:26717201]
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 Flt-3 (unknown origin) B 8.52 pIC50 <3 nM IC50 Eur J Med Chem (2016) 108: 495-504 [PMID:26717201]
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
ChEMBL Inhibition of Axl (unknown origin) B 8.52 pIC50 <3 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]
ChEMBL Competitive inhibition of VEGFR2 (unknown origin) in presence of ATP B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2016) 108: 495-504 [PMID:26717201]
MER proto-oncogene, tyrosine kinase in Human [GtoPdb: 1837] [UniProtKB: Q12866]
GtoPdb - - 7.65 pKi 22.4 nM Ki Exp Mol Med (2022) 54: 1450-1460 [PMID:36056187]
GtoPdb Inhibition at intracellular ATP concentration of 1 mM - 6.89 pIC50 129.9 nM IC50 Exp Mol Med (2022) 54: 1450-1460 [PMID:36056187]

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]