crystal structure of furanopyrimidine 1 bound to lck

File:2of4.gif


2of4, resolution 2.7Å

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OverviewOverview

2,3-Diarylfuro[2,3-b]pyridine-4-amines are a novel class of potent and selective inhibitors of Lck. The discovery, synthesis, and structure activity relationships of this series of inhibitors are reported. The most promising compounds were also profiled to deduce their pharmacokinetic properties.

DiseaseDisease

Known disease associated with this structure: SCID due to LCK deficiency OMIM:[153390]

About this StructureAbout this Structure

2OF4 is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Non-specific protein-tyrosine kinase, with EC number 2.7.10.2 Full crystallographic information is available from OCA.

ReferenceReference

Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties., Martin MW, Newcomb J, Nunes JJ, Bemis JE, McGowan DC, White RD, Buchanan JL, DiMauro EF, Boucher C, Faust T, Hsieh F, Huang X, Lee JH, Schneider S, Turci SM, Zhu X, Bioorg Med Chem Lett. 2007 Apr 15;17(8):2299-304. Epub 2007 Jan 24. PMID:17276681

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