(+)-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 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]
