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ChEMBL ligand: CHEMBL14021 (Antischim b, E-280, E280, Ethanecarboxylic acid, FEMA NO. 2924, INS-280, INS NO.280, Luprosil, Metacetonic acid, Propanoic acid, Propionate, Propionic acid) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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FFA3 receptor/Free fatty acid receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5201] [GtoPdb: 227] [UniProtKB: O14843] | ||||||||
ChEMBL | Agonist activity at human GPCR41 transfected in HEK293 cells assessed as [35S]GTPgammaS binding by scintillation counting method | F | 4.92 | pEC50 | 12000 | nM | EC50 | J Med Chem (2018) 61: 47-61 [PMID:28745893] |
ChEMBL | Agonist activity at human FFA3 receptor stably expressed in Flp-In T-Rex HEK293 cells cotransfected with eYFP assessed as inhibition of forskolin-induced cAMP production measured after 1 hr by fluorescence plate reader assay | F | 4.93 | pEC50 | 11748.98 | nM | EC50 | J Med Chem (2020) 63: 3577-3595 [PMID:32141297] |
ChEMBL | Agonist activity at human FFA3 receptor stably expressed in Flp-In T-Rex HEK293 cell membrane assessed as stimulation of [35S]-GTPgammaS binding measured after 1 hr in presence of GDP by liquid scintillation spectrometry | F | 4.97 | pEC50 | 10715.19 | nM | EC50 | J Med Chem (2020) 63: 3577-3595 [PMID:32141297] |
GtoPdb | - | - | 5.7 | pEC50 | - | - | - |
J Biol Chem (2003) 278: 11312-9 [PMID:12496283]; J Biol Chem (2003) 278: 25481-9 [PMID:12711604]; Proc Natl Acad Sci USA (2004) 101: 1045-50 [PMID:14722361]; J Biol Chem (2011) 286: 10628-40 [PMID:21220428] |
FFA2 receptor in Human [GtoPdb: 226] [UniProtKB: O15552] | ||||||||
GtoPdb | - | - | 4.9 | pEC50 | - | - | - |
J Biol Chem (2003) 278: 11312-9 [PMID:12496283]; Biochem Biophys Res Commun (2003) 303: 1047-52 [PMID:12684041]; J Biol Chem (2003) 278: 25481-9 [PMID:12711604]; J Biol Chem (2011) 286: 10628-40 [PMID:21220428] |
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]