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 | GPCR PRESTO-Tango dose-response in agonist mode with target: FFAR4 | F | 5.33 | pEC50 | 4662.06 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| ChEMBL | Agonist activity at human GPR120 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay | F | 5.85 | pEC50 | 1420 | nM | EC50 | Eur J Med Chem (2023) 251: 115267-115267 [PMID:36933395] |
| 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] |
| FPR3/N-formyl peptide receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR3 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 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]
