TUG-1197 [Ligand Id: 11195] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3941880
  • FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
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  • FFA4 receptor/G-protein coupled receptor 120 in Human [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
  • FFA4 receptor in Mouse [GtoPdb: 127] [UniProtKB: Q7TMA4]
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  • FFA4 receptor in Human [GtoPdb: 127] [UniProtKB: Q5NUL3]
  • FFA4 receptor/Omega-3 fatty acid receptor 1 in Mouse [ChEMBL: CHEMBL2052036] [GtoPdb: 127] [UniProtKB: Q7TMA4]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
ChEMBL Antagonist activity against human FFA1 expressed in human Flp-In T-REx293 cells assessed as as reduction in TUG424-induced response by Fura2-AM dye based calcium mobilization assay F 4 pIC50 >100000 nM IC50 J Med Chem (2016) 59: 8868-8878 [PMID:27570890]
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
GtoPdb Determined in a Ca2+ mobilization assay. - 6.63 pEC50 234 nM EC50 J Med Chem (2016) 59: 8868-8878 [PMID:27570890]
ChEMBL Agonist activity at human FFA4 expressed in human Flp-In T-REx293 cells by Fura2-AM dye based calcium mobilization assay F 6.63 pEC50 234.42 nM EC50 J Med Chem (2016) 59: 8868-8878 [PMID:27570890]
ChEMBL Agonist activity at C-terminal YFP-tagged human FFA4 expressed in HEK293 cells in presence of coelentrazine h by BRET based beta-arrestin-2 interaction assay B 6.89 pEC50 128 nM EC50 J Med Chem (2016) 59: 8868-8878 [PMID:27570890]
ChEMBL Agonist activity at C-terminal YFP-tagged human FFA4 expressed in HEK293 cells in presence of coelentrazine h by BRET based beta-arrestin-2 interaction assay B 6.91 pEC50 123.03 nM EC50 J Med Chem (2016) 59: 8868-8878 [PMID:27570890]
FFA4 receptor in Mouse [GtoPdb: 127] [UniProtKB: Q7TMA4]
GtoPdb Determined in a Ca2+ mobilization assay. - 6.83 pEC50 148 nM EC50 J Med Chem (2016) 59: 8868-8878 [PMID:27570890]
FFA4 receptor in Human [GtoPdb: 127] [UniProtKB: Q5NUL3]
GtoPdb Determined in a Ca2+ mobilization assay. - 6.63 pEC50 234 nM EC50 J Med Chem (2016) 59: 8868-8878 [PMID:27570890]
FFA4 receptor/Omega-3 fatty acid receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2052036] [GtoPdb: 127] [UniProtKB: Q7TMA4]
ChEMBL Agonist activity mouse FFA4 by by BRET based beta-arrestin-2 interaction assay B 6.32 pEC50 478.63 nM EC50 J Med Chem (2016) 59: 8868-8878 [PMID:27570890]
GtoPdb Determined in a Ca2+ mobilization assay. - 6.83 pEC50 148 nM EC50 J Med Chem (2016) 59: 8868-8878 [PMID:27570890]
ChEMBL Agonist activity mouse FFA4 by Gq-dependent calcium mobilization assay F 6.83 pEC50 147.91 nM EC50 J Med Chem (2016) 59: 8868-8878 [PMID:27570890]

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]