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PDBsum entry 3hp5
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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 n-Substituted pyridinones as potent and selective inhibitors of p38 kinase.
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Authors
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S.R.Selness,
R.V.Devraj,
J.B.Monahan,
T.L.Boehm,
J.K.Walker,
B.Devadas,
R.C.Durley,
R.Kurumbail,
H.Shieh,
L.Xing,
M.Hepperle,
P.V.Rucker,
K.D.Jerome,
A.G.Benson,
L.D.Marrufo,
H.M.Madsen,
J.Hitchcock,
T.J.Owen,
L.Christie,
M.A.Promo,
B.S.Hickory,
E.Alvira,
W.Naing,
R.Blevis-Bal.
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Ref.
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Bioorg Med Chem Lett, 2009,
19,
5851-5856.
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PubMed id
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Abstract
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The identification and evolution of a series of potent and selective p38
inhibitors is described. p38 inhibitors based on a N-benzyl pyridinone
high-throughput screening hit were prepared and their SAR explored. Their design
was guided by ligand bound co-crystals of p38alpha. These efforts resulted in
the identification of 12r and 19 as orally active inhibitors of p38 with
significant efficacy in both acute and chronic models of inflammation.
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