TUG-891 [Ligand Id: 6490] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2058533 |
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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 human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay | B | 4.47 | pEC50 | 33884.42 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 127650-127650 [PMID:33127539] |
| 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 | F | 6.33 | pEC50 | 471 | nM | EC50 | ACS Med Chem Lett (2016) 7: 579-583 [PMID:27326330] |
| ChEMBL | Agonist activity at human FFA4 receptor expressed in CHO-K1 cells assessed as increase in amplitude of dynamic mass redistribution response by DMR assay | B | 6.8 | pEC50 | 158.49 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 127650-127650 [PMID:33127539] |
| 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 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]
