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ChEMBL ligand: CHEMBL3785909 (Amg-337, AMG 337) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
GtoPdb | Biochemically assessed value. | - | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6307-12 [PMID:19819693] |
ChEMBL | Inhibition of HGF-mediated MET autophosphorylation in human PC3 cells preincubated for 1 hr followed by stimulation with human HGF measured after 10 mins by electrochemiluminescence immunoassay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2016) 59: 2328-2342 [PMID:26812066] |
ChEMBL | Inhibition of recombinant MET (unknown origin) using gastrin peptide as substrate preincubated for 30 mins followed by substrate addition incubated for 60 mins by HTRF assay | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2016) 59: 2328-2342 [PMID:26812066] |
CYP3A4 in Human [GtoPdb: 1337] [UniProtKB: P08684] | ||||||||
GtoPdb | - | - | 4.3 | pIC50 | 50000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6307-12 [PMID:19819693] |
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]