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Synonyms: MP-10 | PF-02545920 | PF-2545920 | PF2545920 | pyrazole 9 [PMID: 19630403]
Compound class: Synthetic organic
Comment: Mardepodect (PF-2545920) is a selective, orally active inhibitor of phosphodiesterase (PDE) 10A . Identified using structure-based drug design, the compound is optimised for selectivity, brain penetration and drug-like properties. PF-2545920 is the first PDE10A inhibitor identified as a clinical lead utilizing this mechanism for the treatment of schizophrenia.
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. Beaumont V, Zhong S, Lin H, Xu W, Bradaia A, Steidl E, Gleyzes M, Wadel K, Buisson B, Padovan-Neto FE et al.. (2016)
Phosphodiesterase 10A Inhibition Improves Cortico-Basal Ganglia Function in Huntington's Disease Models.
Neuron, 92 (6): 1220-1237. [PMID:27916455]
2. Schmidt CJ, Chapin DS, Cianfrogna J, Corman ML, Hajos M, Harms JF, Hoffman WE, Lebel LA, McCarthy SA, Nelson FR et al.. (2008)
Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia.
J Pharmacol Exp Ther, 325 (2): 681-90. [PMID:18287214]
3. Verhoest PR, Chapin DS, Corman M, Fonseca K, Harms JF, Hou X, Marr ES, Menniti FS, Nelson F, O'Connor R et al.. (2009)
Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia.
J Med Chem, 52 (16): 5188-96. [PMID:19630403]