TUG-891 [Ligand Id: 6490] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2058533
  • 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]
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  • 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 Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay F 4.19 pEC50 64565.42 nM EC50 J. Med. Chem. (2012) 55: 4511-4515 [PMID:22519963]
ChEMBL Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay F 4.28 pEC50 52600 nM EC50 Bioorg Med Chem (2017) 25: 6647-6652 [PMID:29100735]
ChEMBL Agonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assay F 5.3 pEC50 5011.87 nM EC50 J. Med. Chem. (2012) 55: 4511-4515 [PMID:22519963]
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
ChEMBL Agonist activity at GPR120 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay B 6.33 pEC50 471 nM EC50 ACS Med. Chem. Lett. (2016) 7: 579-583 [PMID:27326330]
ChEMBL Agonist activity at GPR120 expressed in Flp-In TREx293 cells by calcium assay F 7.02 pEC50 95.5 nM EC50 J. Med. Chem. (2012) 55: 4511-4515 [PMID:22519963]
ChEMBL Agonist activity at human FFAR4 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by luminescence assay F 7.12 pEC50 75.3 nM EC50 Bioorg Med Chem (2017) 25: 6647-6652 [PMID:29100735]
ChEMBL Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay F 7.36 pEC50 43.65 nM EC50 J. Med. Chem. (2012) 55: 4511-4515 [PMID:22519963]
FFA4 receptor/Omega-3 fatty acid receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2052036] [GtoPdb: 127] [UniProtKB: Q7TMA4]
ChEMBL Agonist activity at mouse GPR120 F 7.77 pEC50 16.98 nM EC50 J. Med. Chem. (2012) 55: 4511-4515 [PMID:22519963]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]