2of4: Difference between revisions

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==Overview==
==Overview==
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.
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.
 
==Disease==
Known disease associated with this structure: SCID due to LCK deficiency OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=153390 153390]]


==About this Structure==
==About this Structure==
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==Reference==
==Reference==
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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17276681 17276681]
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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17276681 17276681]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Non-specific protein-tyrosine kinase]]
[[Category: Non-specific protein-tyrosine kinase]]
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Martin, M.W.]]
[[Category: Martin, M W.]]
[[Category: 979]]
[[Category: 979]]
[[Category: kinase domain]]
[[Category: kinase domain]]
[[Category: lck]]
[[Category: lck]]


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Revision as of 19:17, 21 February 2008

File:2of4.gif


2of4, resolution 2.7Å

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crystal structure of furanopyrimidine 1 bound to lck

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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