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PDBsum entry 4ff8
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Transferase/transferase inhibitor
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PDB id
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4ff8
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References listed in PDB file
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Key reference
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Title
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Highly selective 2,4-Diaminopyrimidine-5-Carboxamide inhibitors of sky kinase.
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Authors
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N.A.Powell,
J.K.Hoffman,
F.L.Ciske,
M.D.Kaufman,
J.T.Kohrt,
J.Quin,
D.J.Sheehan,
A.Delaney,
S.M.Baxi,
C.Catana,
P.Mcconnell,
J.Ohren,
L.A.Perrin,
J.J.Edmunds.
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Ref.
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Bioorg Med Chem Lett, 2013,
23,
1046-1050.
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PubMed id
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Abstract
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We report the SAR around a series of 2,4-diaminopyrimidine-5-carboxamide
inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency
but moderate kinase selectivity, while 2-aminobenzyl analogs that fill the
Ala571 subpocket exhibit good inhibition activity and excellent kinase
selectivity.
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