Synonyms: MK 0364 | MK-0364
Compound class:
Synthetic organic
Comment: Taranabant is a cannabinoid CB1 receptor antagonist/inverse agonist [2-3], with anorectic action. It was investigated for its potential as a novel weight management therapeutic in obese and overweight patients.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Addy C, Wright H, Van Laere K, Gantz I, Erondu N, Musser BJ, Lu K, Yuan J, Sanabria-Bohórquez SM, Stoch A et al.. (2008)
The acyclic CB1R inverse agonist taranabant mediates weight loss by increasing energy expenditure and decreasing caloric intake. Cell Metab, 7 (1): 68-78. [PMID:18177726] |
2. Foloppe N, Benwell K, Brooks TD, Kennett G, Knight AR, Misra A, Monck NJ. (2009)
Discovery and functional evaluation of diverse novel human CB(1) receptor ligands. Bioorg Med Chem Lett, 19 (15): 4183-90. [PMID:19520572] |
3. Lin LS, Ha S, Ball RG, Tsou NN, Castonguay LA, Doss GA, Fong TM, Shen CP, Xiao JC, Goulet MT et al.. (2008)
Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist. J Med Chem, 51 (7): 2108-14. [PMID:18333607] |