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PDBsum entry 4rx9
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Transferase/transferase inhibitor
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PDB id
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4rx9
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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 and profiling of a selective and efficacious syk inhibitor.
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Authors
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G.Thoma,
A.B.Smith,
M.J.Van eis,
E.Vangrevelinghe,
J.Blanz,
R.Aichholz,
A.Littlewood-Evans,
C.C.Lee,
H.Liu,
H.G.Zerwes.
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Ref.
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J Med Chem, 2015,
58,
1950-1963.
[DOI no: ]
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PubMed id
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Abstract
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We describe the discovery of selective and potent Syk inhibitor 11, which
exhibited favorable PK profiles in rat and dog and was found to be active in a
collagen-induced arthritis model in rats. Compound 11 was selected for further
profiling, but, unfortunately, in GLP toxicological studies it showed liver
findings in rat and dog. Nevertheless, 11 could become a valuable tool compound
to investigate the rich biology of Syk in vitro and in vivo.
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