AMG7703 [Ligand Id: 5803] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL594671
  • FFA2 receptor/Free fatty acid receptor 2 in Human [ChEMBL: CHEMBL5493] [GtoPdb: 226] [UniProtKB: O15552]
  • FFA2 receptor/Free fatty acid receptor 2 in Mouse [ChEMBL: CHEMBL3309047] [GtoPdb: 226] [UniProtKB: Q8VCK6]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
FFA2 receptor/Free fatty acid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5493] [GtoPdb: 226] [UniProtKB: O15552]
ChEMBL Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production F 6.15 pIC50 700 nM IC50 Bioorg Med Chem Lett (2010) 20: 493-498 [PMID:20005104]
GtoPdb - - 6.35 pEC50 450 nM EC50 Mol Pharmacol (2008) 74: 1599-609 [PMID:18818303];
Mol Pharmacol (2011) 80: 163-73 [PMID:21498659]
ChEMBL Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay F 6.38 pEC50 416.87 nM EC50 J Med Chem (2018) 61: 9534-9550 [PMID:30247908]
ChEMBL Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method F 7 pEC50 100 nM EC50 Bioorg Med Chem (2018) 26: 5169-5180 [PMID:30253886]
FFA2 receptor/Free fatty acid receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3309047] [GtoPdb: 226] [UniProtKB: Q8VCK6]
ChEMBL Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method F 6.8 pEC50 158.49 nM EC50 Bioorg Med Chem (2018) 26: 5169-5180 [PMID:30253886]

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]