acifran [Ligand Id: 1595] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL278488 (Acifran, Acifranum, AY-25,712, AY-25712, Reductol) |
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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 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]
