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PDBsum entry 3gwt
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References listed in PDB file
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Key reference
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Title
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Quinolines as a novel structural class of potent and selective pde4 inhibitors. Optimisation for inhaled administration.
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Authors
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M.D.Woodrow,
S.P.Ballantine,
M.D.Barker,
B.J.Clarke,
J.Dawson,
T.W.Dean,
C.J.Delves,
B.Evans,
S.L.Gough,
S.B.Guntrip,
S.Holman,
D.S.Holmes,
M.Kranz,
M.K.Lindvaal,
F.S.Lucas,
M.Neu,
L.E.Ranshaw,
Y.E.Solanke,
D.O.Somers,
P.Ward,
J.O.Wiseman.
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Ref.
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Bioorg Med Chem Lett, 2009,
19,
5261-5265.
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PubMed id
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Abstract
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Crystallography driven optimisation of a lead derived from similarity searching
of the GSK compound collection resulted in the discovery of
quinoline-3-carboxamides as highly potent and selective inhibitors of
phosphodiesterase 4B. This series has been optimized to GSK256066, a potent
PDE4B inhibitor which also inhibits LPS induced production of TNF-alpha from
isolated human peripheral blood mononuclear cells with a pIC(50) of 11.1.
GSK256066 also has a suitable profile for inhaled dosing.
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