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PDBsum entry 3e63
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References listed in PDB file
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Key reference
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Title
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Fragment-Based discovery of jak-2 inhibitors.
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Authors
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S.Antonysamy,
G.Hirst,
F.Park,
P.Sprengeler,
F.Stappenbeck,
R.Steensma,
M.Wilson,
M.Wong.
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Ref.
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Bioorg Med Chem Lett, 2009,
19,
279-282.
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PubMed id
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Abstract
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Fragment-based hit identification coupled with crystallographically enabled
structure-based drug design was used to design potent inhibitors of JAK-2. After
two iterations from fragment 1, we were able to increase potency by greater than
500-fold to provide sulfonamide 13, a 78-nM JAK-2 inhibitor.
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