5-butyl-1H-pyrazole-3-carboxylic acid [Ligand Id: 1591] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL428730
  • 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]
  • HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Rat [ChEMBL: CHEMBL4731] [GtoPdb: 312] [UniProtKB: Q80Z39]
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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 Agonist activity at human GPR109b expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay F 4.93 pEC50 11748.98 nM EC50 Bioorg Med Chem Lett (2007) 17: 5620-5623 [PMID:17804224]
HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3785] [GtoPdb: 312] [UniProtKB: Q8TDS4]
ChEMBL Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test F 5.85 pEC50 1400 nM EC50 Bioorg Med Chem Lett (2007) 17: 4914-4919 [PMID:17588745]
ChEMBL Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay F 6 pEC50 >1000 nM EC50 Bioorg Med Chem Lett (2007) 17: 5620-5623 [PMID:17804224]
ChEMBL Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay F 7.07 pEC50 85.11 nM EC50 Bioorg Med Chem Lett (2007) 17: 5620-5623 [PMID:17804224]
HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4731] [GtoPdb: 312] [UniProtKB: Q80Z39]
GtoPdb - - 7.1 pKi - - - J Med Chem (2003) 46: 3945-51 [PMID:12930155]
ChEMBL Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane. B 7.14 pKi 72 nM Ki J Med Chem (2003) 46: 3945-3951 [PMID:12930155]

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]