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PDBsum entry 4zim
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Transferase/transferase inhibitor
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PDB id
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4zim
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References listed in PDB file
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Key reference
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Title
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9h-Carbazole-1-Carboxamides as potent and selective jak2 inhibitors.
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Authors
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K.Zimmermann,
X.Sang,
H.A.Mastalerz,
W.L.Johnson,
G.Zhang,
Q.Liu,
D.Batt,
L.J.Lombardo,
D.Vyas,
G.L.Trainor,
J.S.Tokarski,
M.V.Lorenzi,
D.You,
M.M.Gottardis,
J.Lippy,
J.Khan,
J.S.Sack,
A.V.Purandare.
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Ref.
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Bioorg Med Chem Lett, 2015,
25,
2809-2812.
[DOI no: ]
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PubMed id
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Abstract
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The discovery, synthesis, and characterization of 9H-carbazole-1-carboxamides as
potent and selective ATP-competitive inhibitors of Janus kinase 2 (JAK2) are
discussed. Optimization for JAK family selectivity led to compounds 14 and 21,
with greater than 45-fold selectivity for JAK2 over all other members of the JAK
kinase family.
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