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Synonyms: compound 8 [PMID: 26509551] | PF06282999
Compound class: Synthetic organic
Comment: PF-06282999 is a thiouracil-based, irreversible mechanism-based, investigational myeloperoxidase (MPO) inhibitor  that was advanced as a clinical candidate, primarily as a novel treatment for cardiovascular diseases .
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. Dong JQ, Varma MV, Wolford A, Ryder T, Di L, Feng B, Terra SG, Sagawa K, Kalgutkar AS. (2016)
Pharmacokinetics and Disposition of the Thiouracil Derivative PF-06282999, an Orally Bioavailable, Irreversible Inactivator of Myeloperoxidase Enzyme, Across Animals and Humans.
Drug Metab Dispos, 44 (2): 209-19. [PMID:26608081]
2. Ruggeri RB, Buckbinder L, Bagley SW, Carpino PA, Conn EL, Dowling MS, Fernando DP, Jiao W, Kung DW, Orr ST et al.. (2015)
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
J Med Chem, 58 (21): 8513-28. [PMID:26509551]