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