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PDBsum entry 3b2w
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References listed in PDB file
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Key reference
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Title
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N-(3-(Phenylcarbamoyl)arylpyrimidine)-5-Carboxamides as potent and selective inhibitors of lck: structure, Synthesis and sar.
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Authors
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H.L.Deak,
J.R.Newcomb,
J.J.Nunes,
C.Boucher,
A.C.Cheng,
E.F.Dimauro,
L.F.Epstein,
P.Gallant,
B.L.Hodous,
X.Huang,
J.H.Lee,
V.F.Patel,
S.Schneider,
S.M.Turci,
X.Zhu.
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Ref.
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Bioorg Med Chem Lett, 2008,
18,
1172-1176.
[DOI no: ]
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PubMed id
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Abstract
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N-3-(Phenylcarbamoyl)arylpyrimidine-5-carboxamides are a novel class of
selective Lck inhibitors. This series of compounds derives its selectivity from
a hydrogen bond with the gatekeeper Thr316 of the enzyme. X-ray co-crystal
structural data, structure-activity relationships, and the synthesis of these
inhibitors are reported herein.
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