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PDBsum entry 4xj0
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Transferase/transferase inhibitor
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PDB id
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4xj0
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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 highly potent, Selective, And efficacious small molecule inhibitors of erk1/2.
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Authors
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L.Ren,
J.Grina,
D.Moreno,
J.F.Blake,
J.J.Gaudino,
R.Garrey,
A.T.Metcalf,
M.Burkard,
M.Martinson,
K.Rasor,
H.Chen,
B.Dean,
S.E.Gould,
P.Pacheco,
S.Shahidi-Latham,
J.Yin,
K.West,
W.Wang,
J.G.Moffat,
J.B.Schwarz.
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Ref.
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J Med Chem, 2015,
58,
1976-1991.
[DOI no: ]
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PubMed id
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Abstract
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Using structure-based design, a novel series of pyridone ERK1/2 inhibitors was
developed. Optimization led to the identification of (S)-14k, a potent,
selective, and orally bioavailable agent that inhibited tumor growth in mouse
xenograft models. On the basis of its in vivo efficacy and preliminary safety
profiles, (S)-14k was selected for further preclinical evaluation.
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