 |
PDBsum entry 5em7
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Transferase/transferase inhibitor
|
PDB id
|
|
|
|
5em7
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
References listed in PDB file
|
|
|
Key reference
|
|
|
Title
|
|
Pyridones as highly selective, Noncovalent inhibitors of t790m double mutants of egfr.
|
|
|
Authors
|
|
M.C.Bryan,
D.J.Burdick,
B.K.Chan,
Y.Chen,
S.Clausen,
J.Dotson,
C.Eigenbrot,
R.Elliott,
E.J.Hanan,
R.Heald,
P.Jackson,
H.La,
M.Lainchbury,
S.Malek,
S.E.Mann,
H.E.Purkey,
G.Schaefer,
S.Schmidt,
E.Seward,
S.Sideris,
S.Wang,
I.Yen,
C.Yu,
T.P.Heffron.
|
|
|
Ref.
|
|
Acs Med Chem Lett, 2016,
7,
100-104.
[DOI no: ]
|
|
|
PubMed id
|
|
|
|
|
|
Abstract
|
|
|
The rapid advancement of a series of noncovalent inhibitors of T790M mutants of
EGFR is discussed. The optimization of pyridone 1, a nonselective
high-throughput screening hit, to potent molecules with high levels of
selectivity over wtEGFR and the broader kinome is described herein.
|
|
|
|
|
|
|
