title: Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
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.
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Marian C
authors.initials: MC
authors.lastname: Bryan
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Daniel J
authors.initials: DJ
authors.lastname: Burdick
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Bryan K
authors.initials: BK
authors.lastname: Chan
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Chen
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Saundra
authors.initials: S
authors.lastname: Clausen
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Jennafer
authors.initials: J
authors.lastname: Dotson
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Charles
authors.initials: C
authors.lastname: Eigenbrot
authors.affiliation: Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
authors.forename: Richard
authors.initials: R
authors.lastname: Elliott
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Emily J
authors.initials: EJ
authors.lastname: Hanan
authors.affiliation: Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
authors.forename: Robert
authors.initials: R
authors.lastname: Heald
authors.affiliation: Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
authors.forename: Philip
authors.initials: P
authors.lastname: Jackson
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Hank
authors.initials: H
authors.lastname: La
authors.affiliation: Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
authors.forename: Michael
authors.initials: M
authors.lastname: Lainchbury
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Shiva
authors.initials: S
authors.lastname: Malek
authors.affiliation: Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
authors.forename: Sam E
authors.initials: SE
authors.lastname: Mann
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Hans E
authors.initials: HE
authors.lastname: Purkey
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Gabriele
authors.initials: G
authors.lastname: Schaefer
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Stephen
authors.initials: S
authors.lastname: Schmidt
authors.affiliation: Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
authors.forename: Eileen
authors.initials: E
authors.lastname: Seward
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Steve
authors.initials: S
authors.lastname: Sideris
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Shumei
authors.initials: S
authors.lastname: Wang
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Ivana
authors.initials: I
authors.lastname: Yen
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Christine
authors.initials: C
authors.lastname: Yu
authors.affiliation: Genentech , South San Francisco, California 94080, United States.
authors.forename: Timothy P
authors.initials: TP
authors.lastname: Heffron
keywords: Mutant EGFR; T790M; noncovalent; pyridone
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