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PDBsum entry 3l8v
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References listed in PDB file
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Key reference
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Title
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Design, Synthesis and structure-Activity relationships of novel biarylamine-Based met kinase inhibitors.
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Authors
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D.K.Williams,
X.T.Chen,
C.Tarby,
R.Kaltenbach,
Z.W.Cai,
J.S.Tokarski,
Y.An,
J.S.Sack,
B.Wautlet,
J.Gullo-Brown,
B.J.Henley,
R.Jeyaseelan,
K.Kellar,
V.Manne,
G.L.Trainor,
L.J.Lombardo,
J.Fargnoli,
R.M.Borzilleri.
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Ref.
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Bioorg Med Chem Lett, 2010,
20,
2998-3002.
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PubMed id
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Abstract
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Biarylamine-based inhibitors of Met kinase have been identified. Lead compounds
demonstrate nanomolar potency in Met kinase biochemical assays and significant
activity in the Met-driven GTL-16 human gastric carcinoma cell line. X-ray
crystallography revealed that these compounds adopt a bioactive conformation, in
the kinase domain, consistent with that previously seen with 2-pyridone-based
Met kinase inhibitors. Compound 9b demonstrated potent in vivo antitumor
activity in the GTL-16 human tumor xenograft model.
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