(+)-5-(5-bromothiophen-3-yl)-5-methyl-4-oxo-4,5-dihydro-furan-2-carboxylic acid [Ligand Id: 1589] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL375493 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| HCA3 receptor/HM74 nicotinic acid GPCR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4421] [GtoPdb: 313] [UniProtKB: P49019] | ||||||||
| ChEMBL | Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation | F | 5.82 | pEC50 | 1500 | nM | EC50 | J Med Chem (2007) 50: 1445-1448 [PMID:17358052] |
| ChEMBL | Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production | F | 5.83 | pEC50 | 1470 | nM | EC50 | J Med Chem (2008) 51: 7653-7662 [PMID:18983141] |
| ChEMBL | Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation | F | 6.43 | pEC50 | 370 | nM | EC50 | J Med Chem (2007) 50: 1445-1448 [PMID:17358052] |
| HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3785] [GtoPdb: 312] [UniProtKB: Q8TDS4] | ||||||||
| ChEMBL | Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2007) 50: 1445-1448 [PMID:17358052] |
| ChEMBL | Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2008) 51: 7653-7662 [PMID:18983141] |
| GtoPdb | - | - | 7.3 | pEC50 | - | - | - |
J Med Chem (2007) 50: 1445-8 [PMID:17358052]; J Biol Chem (2005) 280: 26649-52 [PMID:15929991] |
| ChEMBL | Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation | F | 7.32 | pEC50 | 48 | nM | EC50 | J Med Chem (2007) 50: 1445-1448 [PMID:17358052] |
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]
