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PDBsum entry 4i0s
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Transferase/transferase inhibitor
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PDB id
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4i0s
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References listed in PDB file
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Key reference
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Title
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Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.
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Authors
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F.Padilla,
N.Bhagirath,
S.Chen,
E.Chiao,
D.M.Goldstein,
J.C.Hermann,
J.Hsu,
J.J.Kennedy-Smith,
A.Kuglstatter,
C.Liao,
W.Liu,
L.E.Lowrie,
K.C.Luk,
S.M.Lynch,
J.Menke,
L.Niu,
T.D.Owens,
C.O-Yang,
A.Railkar,
R.C.Schoenfeld,
M.Slade,
S.Steiner,
Y.C.Tan,
A.G.Villaseñor,
C.Wang,
J.Wanner,
W.Xie,
D.Xu,
X.Zhang,
M.Zhou,
M.C.Lucas.
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Ref.
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J Med Chem, 2013,
56,
1677-1692.
[DOI no: ]
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PubMed id
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Abstract
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We describe the discovery of several pyrrolopyrazines as potent and selective
Syk inhibitors and the efforts that eventually led to the desired improvements
in physicochemical properties and human whole blood potencies. Ultimately, our
mouse model revealed unexpected toxicity that precluded us from further
advancing this series.
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