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PDBsum entry 3ekn
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References listed in PDB file
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Key reference
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Title
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Optimization of 4,6-Bis-Anilino-1h-Pyrrolo[2,3-D]pyrimidine igf-1r tyrosine kinase inhibitors towards jnk selectivity.
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Authors
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S.D.Chamberlain,
A.M.Redman,
J.W.Wilson,
F.Deanda,
J.B.Shotwell,
R.Gerding,
H.Lei,
B.Yang,
K.L.Stevens,
A.M.Hassell,
L.M.Shewchuk,
M.A.Leesnitzer,
J.L.Smith,
P.Sabbatini,
C.Atkins,
A.Groy,
J.L.Rowand,
R.Kumar,
R.A.Mook,
G.Moorthy,
S.Patnaik.
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Ref.
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Bioorg Med Chem Lett, 2009,
19,
360-364.
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PubMed id
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Abstract
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The SAR of C5' functional groups with terminal basic amines at the C6 aniline of
4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines is reported. Examples demonstrate
potent inhibition of IGF-1R with 1000-fold selectivity over JNK1 and 3 in
enzymatic assays.
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