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ChEMBL ligand: CHEMBL456145 (MK-0354) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3785] [GtoPdb: 312] [UniProtKB: Q8TDS4] | ||||||||
ChEMBL | Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells | B | 6.3 | pKi | 505 | nM | Ki | J Med Chem (2008) 51: 5101-5108 [PMID:18665582] |
ChEMBL | Displacement of [3H]nicotinic acid from human GPR109a receptor | B | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2121-2124 [PMID:19307116] |
ChEMBL | Displacement of [3H]nicotinic acid from human GPR10a receptor | B | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4472-4474 [PMID:20615702] |
ChEMBL | Agonist activity against human GPR109a assessed as GTPgammaS binding | F | 5.64 | pEC50 | 2300 | nM | EC50 | J Med Chem (2008) 51: 5101-5108 [PMID:18665582] |
GtoPdb | - | - | 5.78 | pEC50 | 1650 | nM | EC50 | J Med Chem (2008) 51: 5101-8 [PMID:18665582] |
ChEMBL | Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation | F | 5.78 | pEC50 | 1650 | nM | EC50 | J Med Chem (2008) 51: 5101-5108 [PMID:18665582] |
ChEMBL | Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay | F | 6.54 | pEC50 | 286 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2797-2800 [PMID:20363624] |
ChEMBL | Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay | F | 6.54 | pEC50 | 286 | nM | EC50 | J Med Chem (2012) 55: 3644-3666 [PMID:22435740] |
HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4420] [GtoPdb: 312] [UniProtKB: Q9EP66] | ||||||||
ChEMBL | Displacement of [3H]nicotinic acid from mouse GPR109a receptor | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2121-2124 [PMID:19307116] |
ChEMBL | Displacement of [3H]nicotinic acid from mouse GPR10a receptor | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4472-4474 [PMID:20615702] |
ChEMBL | Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation | F | 5.97 | pEC50 | 1080 | nM | EC50 | J Med Chem (2008) 51: 5101-5108 [PMID:18665582] |
ChEMBL | Agonist activity against mouse GPR109a assessed as GTPgammaS binding | F | 6.4 | pEC50 | 400 | nM | EC50 | J Med Chem (2008) 51: 5101-5108 [PMID:18665582] |
HCA2 receptor/Hydroxycarboxylic acid receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4731] [GtoPdb: 312] [UniProtKB: Q80Z39] | ||||||||
ChEMBL | Agonist activity against rat GPR109a assessed as GTPgammaS binding | F | 5.64 | pEC50 | 2300 | nM | EC50 | J Med Chem (2008) 51: 5101-5108 [PMID:18665582] |
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]