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PDBsum entry 5imx
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Transferase/transferase inhibitor
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PDB id
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5imx
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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 and synthesis of novel 3-Sulfonylpyrazol-4-Amino pyrimidines as potent anaplastic lymphoma kinase (alk) inhibitors.
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Authors
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P.Zhang,
J.Dong,
B.Zhong,
D.Zhang,
H.Yuan,
C.Jin,
X.Xu,
H.Li,
Y.Zhou,
Z.Liang,
M.Ji,
T.Xu,
G.Song,
L.Zhang,
G.Chen,
X.Meng,
D.Sun,
J.Shih,
R.Zhang,
G.Hou,
C.Wang,
Y.Jin,
Q.Yang.
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Ref.
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Bioorg Med Chem Lett, 2016,
26,
1910-1918.
[DOI no: ]
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PubMed id
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Abstract
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Anaplastic lymphoma kinase (ALK) is a highly attractive therapeutic target for
the treatment of some non-small cell lung cancer patients. This Letter describes
the further SAR exploration on the novel 3-sulfonylpyrazol-4-amino pyrimidine
scaffold. This work identified a compound 53 with very good in vitro/in vivo
efficacies, good DMPK properties together with better hERG tolerability and it
is currently being profiled for the evaluation as a potential pre-clinical
candidate.
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