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PDBsum entry 3lpb
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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 and sar of potent, Orally available 2,8-Diaryl-Quinoxalines as a new class of jak2 inhibitors.
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Authors
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C.Pissot-Soldermann,
M.Gerspacher,
P.Furet,
C.Gaul,
P.Holzer,
C.Mccarthy,
T.Radimerski,
C.H.Regnier,
F.Baffert,
P.Drueckes,
G.A.Tavares,
E.Vangrevelinghe,
F.Blasco,
G.Ottaviani,
F.Ossola,
J.Scesa,
J.Reetz.
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Ref.
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Bioorg Med Chem Lett, 2010,
20,
2609-2613.
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PubMed id
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Abstract
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We have designed and synthesized a novel series of 2,8-diaryl-quinoxalines as
Janus kinase 2 inhibitors. Many of the inhibitors show low nanomolar activity
against JAK2 and potently suppress proliferation of SET-2 cells in vitro. In
addition, compounds from this series have favorable rat pharmacokinetic
properties suitable for in vivo efficacy evaluation.
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