AMG7703 [Ligand Id: 5803] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL594671 |
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| 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 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]
