TUG-424 [Ligand Id: 3952] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL449588 (4-(2-Toluylethynyl)Dihydrocinnamic Acid) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| apelin receptor/Apelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628481] [GtoPdb: 36] [UniProtKB: P35414] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: APLNR | F | 6.49 | pIC50 | 324.85 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| FPR1/Formyl peptide receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR1 | F | 5.89 | pIC50 | 1279.16 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842] | ||||||||
| ChEMBL | Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay | B | 6.2 | pKi | 630.96 | nM | Ki | J Med Chem (2016) 59: 4849-4858 [PMID:27074625] |
| ChEMBL | Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay | B | 7.17 | pEC50 | 67.61 | nM | EC50 | J Med Chem (2016) 59: 4849-4858 [PMID:27074625] |
| ChEMBL | Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis | F | 7.34 | pEC50 | 46 | nM | EC50 | J Med Chem (2013) 56: 982-992 [PMID:23294321] |
| ChEMBL | Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry | F | 7.34 | pEC50 | 45.71 | nM | EC50 | J Med Chem (2011) 54: 6691-6703 [PMID:21854074] |
| ChEMBL | Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay | F | 7.34 | pEC50 | 45.71 | nM | EC50 | ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558] |
| ChEMBL | Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay | F | 7.49 | pEC50 | 32.36 | nM | EC50 | J Med Chem (2008) 51: 7061-7064 [PMID:18947221] |
| ChEMBL | Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay | F | 7.49 | pEC50 | 32 | nM | EC50 | J Med Chem (2008) 51: 7061-7064 [PMID:18947221] |
| GtoPdb | - | - | 7.5 | pEC50 | - | - | - | J Med Chem (2008) 51: 7061-4 [PMID:18947221] |
| FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3] | ||||||||
| ChEMBL | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | F | 5.65 | pEC50 | 2238.72 | nM | EC50 | J Med Chem (2012) 55: 4511-4515 [PMID:22519963] |
| ChEMBL | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | B | 5.84 | pEC50 | 1445.44 | nM | EC50 | ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558] |
| GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183 | F | 6.23 | pIC50 | 582.5 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: CHRM2 | F | 6.22 | pIC50 | 602.2 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 | 5.85 | pIC50 | 1427.99 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR65/Psychosine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714081] [GtoPdb: 113] [UniProtKB: Q8IYL9] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR65 | F | 6.44 | pIC50 | 364.84 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| S1P1 receptor/Sphingosine 1-phosphate receptor Edg-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: S1PR1 | F | 6.6 | pIC50 | 248.92 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
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]
