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Synonyms: compound 3 [PMID: 25565255]
Compound class: Synthetic organic
Comment: CTEP is a negative allosteric modulator (NAM) of the glutamate metabotropic receptor 5 (mGlu5) GPCR [1-2]. Structurally, CTEP and basimglurant and are analogues. CTEP has a notably longer half-life in rodents (49 hours) than basimglurant (~10 hours), so is better suited for rodents studies requiring chronic exposure/treatment.
Ligand Activity Visualisation Charts
These 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.✖
1. Jaeschke G, Kolczewski S, Spooren W, Vieira E, Bitter-Stoll N, Boissin P, Borroni E, Büttelmann B, Ceccarelli S, Clemann N et al.. (2015)
Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
J Med Chem, 58 (3): 1358-71. [PMID:25565255]
2. Lindemann L, Jaeschke G, Michalon A, Vieira E, Honer M, Spooren W, Porter R, Hartung T, Kolczewski S, Büttelmann B et al.. (2011)
CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.
J Pharmacol Exp Ther, 339 (2): 474-86. [PMID:21849627]