5-butyl-1H-pyrazole-3-carboxylic acid [Ligand Id: 1591] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL428730 |
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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 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]
