acifran [Ligand Id: 1595] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL278488 (Acifran, Reductol, AY-25712)
  • HCA3 receptor/HM74 nicotinic acid GPCR in Human [ChEMBL: CHEMBL4421] [GtoPdb: 313] [UniProtKB: P49019]
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  • HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Human [ChEMBL: CHEMBL3785] [GtoPdb: 312] [UniProtKB: Q8TDS4]
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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 assessed as inhibition of forskolin-stimulated cAMP production F 5.52 pIC50 3000 nM IC50 J. Med. Chem. (2008) 51: 7653-7662 [PMID:18983141]
GtoPdb - - 5.2 pEC50 - - - J. Biol. Chem. (2003) 278: 9869-74 [PMID:12522134];
Biochem. Biophys. Res. Commun. (2006) 340: 482-90 [PMID:16389067];
J. Med. Chem. (2007) 50: 1445-8 [PMID:17358052];
J. Biol. Chem. (2005) 280: 26649-52 [PMID:15929991]
ChEMBL Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation F 5.38 pEC50 4200 nM EC50 J. Med. Chem. (2007) 50: 1445-1448 [PMID:17358052]
ChEMBL Activity at GPR109b assessed as inhibition of forskolin-stimulated cAMP production F 5.38 pEC50 4200 nM EC50 J. Med. Chem. (2008) 51: 7653-7662 [PMID:18983141]
ChEMBL Agonist activity at N-terminal HA-tagged GPR109b receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay F 5.38 pEC50 4200 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 4207-4209 [PMID:19524438]
ChEMBL Activity at GPR109b in CHO cells assessed as inhibition of forskolin-induced cAMP generation F 5.52 pEC50 3000 nM EC50 J. Med. Chem. (2007) 50: 1445-1448 [PMID:17358052]
ChEMBL Agonist activity at HCA3 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA B 6.5 pEC50 316 nM EC50 Bioorg. Med. Chem. (2015) 23: 4013-4025 [PMID:25737085]
HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3785] [GtoPdb: 312] [UniProtKB: Q8TDS4]
ChEMBL Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production F 6.3 pIC50 500 nM IC50 J. Med. Chem. (2008) 51: 7653-7662 [PMID:18983141]
ChEMBL Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation F 5.89 pEC50 1300 nM EC50 J. Med. Chem. (2007) 50: 1445-1448 [PMID:17358052]
ChEMBL Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production F 5.89 pEC50 1300 nM EC50 J. Med. Chem. (2008) 51: 7653-7662 [PMID:18983141]
ChEMBL Agonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay F 5.89 pEC50 1300 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 4207-4209 [PMID:19524438]
GtoPdb - - 5.9 pEC50 - - - J. Biol. Chem. (2003) 278: 9869-74 [PMID:12522134];
Biochem. Biophys. Res. Commun. (2006) 340: 482-90 [PMID:16389067];
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 6.28 pEC50 520 nM EC50 J. Med. Chem. (2007) 50: 1445-1448 [PMID:17358052]
ChEMBL Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA B 6.8 pEC50 160 nM EC50 Bioorg. Med. Chem. (2015) 23: 4013-4025 [PMID:25737085]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]