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PDBsum entry 3cp9
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References listed in PDB file
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Key reference
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Title
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Discovery of aryl aminoquinazoline pyridones as potent, Selective, And orally efficacious inhibitors of receptor tyrosine kinase c-Kit.
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Authors
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E.Hu,
A.Tasker,
R.D.White,
R.K.Kunz,
J.Human,
N.Chen,
R.Bürli,
R.Hungate,
P.Novak,
A.Itano,
X.Zhang,
V.Yu,
Y.Nguyen,
Y.Tudor,
M.Plant,
S.Flynn,
Y.Xu,
K.L.Meagher,
D.A.Whittington,
G.Y.Ng.
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Ref.
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J Med Chem, 2008,
51,
3065-3068.
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PubMed id
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Abstract
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Inhibition of c-Kit has the potential to treat mast cell associated fibrotic
diseases. We report the discovery of several aminoquinazoline pyridones that are
potent inhibitors of c-Kit with greater than 200-fold selectivity against KDR,
p38, Lck, and Src. In vivo efficacy of pyridone 16 by dose-dependent inhibition
of histamine release was demonstrated in a rodent pharmacodynamic model of mast
cell activation.
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