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PDBsum entry 5vgo
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Transferase/transferase inhibitor
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PDB id
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5vgo
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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 of potent and selective tricyclic inhibitors of bruton'S tyrosine kinase with improved druglike properties.
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Authors
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X.Wang,
J.Barbosa,
P.Blomgren,
M.C.Bremer,
J.Chen,
J.J.Crawford,
W.Deng,
L.Dong,
C.Eigenbrot,
S.Gallion,
J.Hau,
H.Hu,
A.R.Johnson,
A.Katewa,
J.E.Kropf,
S.H.Lee,
L.Liu,
J.W.Lubach,
J.Macaluso,
P.Maciejewski,
S.A.Mitchell,
D.F.Ortwine,
J.Dipaolo,
K.Reif,
H.Scheerens,
A.Schmitt,
H.Wong,
J.M.Xiong,
J.Xu,
Z.Zhao,
F.Zhou,
K.S.Currie,
W.B.Young.
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Ref.
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ACS Med Chem Lett, 2017,
8,
608-613.
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PubMed id
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Abstract
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In our continued effort to discover and develop best-in-class Bruton's tyrosine
kinase (Btk) inhibitors for the treatment of B-cell lymphomas, rheumatoid
arthritis, and systemic lupus erythematosus, we devised a series of novel
tricyclic compounds that improved upon the druglike properties of our previous
chemical matter. Compounds exemplified byG-744are highly potent,
selective for Btk, metabolically stable, well tolerated, and efficacious in an
animal model of arthritis.
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