MK 0354 [Ligand Id: 5784] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
