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Synonyms: compound 30 [PMID: 29293004] | PF 05180999 | PF-999 | PF05180999
Compound class: Synthetic organic
Comment: PF-05180999 is a selective and brain-penetrant inhibitor of phosphodiesterase 2A (PDE2A) [1-2]. Its intended clinical utility was to target cognitive impairment associated with 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. Helal CJ, Arnold E, Boyden T, Chang C, Chappie TA, Fisher E, Hajos M, Harms JF, Hoffman WE, Humphrey JM et al.. (2018)
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
J Med Chem, 61 (3): 1001-1018. [PMID:29293004]
2. Mikami S, Sasaki S, Asano Y, Ujikawa O, Fukumoto S, Nakashima K, Oki H, Kamiguchi N, Imada H, Iwashita H et al.. (2017)
Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.
J Med Chem, 60 (18): 7658-7676. [PMID:28759228]