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PDBsum entry 4x7l
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Transferase/transferase inhibitor
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PDB id
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4x7l
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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 1h-Pyrazol-3(2h)-Ones as potent and selective inhibitors of protein kinase r-Like endoplasmic reticulum kinase (perk).
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Authors
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A.L.Smith,
K.L.Andrews,
H.Beckmann,
S.F.Bellon,
P.J.Beltran,
S.Booker,
H.Chen,
Y.A.Chung,
N.D.D'Angelo,
J.Dao,
K.R.Dellamaggiore,
P.Jaeckel,
R.Kendall,
K.Labitzke,
A.M.Long,
S.Materna-Reichelt,
P.Mitchell,
M.H.Norman,
D.Powers,
M.Rose,
P.L.Shaffer,
M.M.Wu,
J.R.Lipford.
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Ref.
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J Med Chem, 2015,
58,
1426-1441.
[DOI no: ]
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PubMed id
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Abstract
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The structure-based design and optimization of a novel series of selective PERK
inhibitors are described resulting in the identification of 44 as a potent,
highly selective, and orally active tool compound suitable for PERK pathway
biology exploration both in vitro and in vivo.
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