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 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]