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Discovery of N-(1-Acryloylazetidin-3-yl)-2-(1H-indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C.
Shin, Youngsook; Jeong, Joon Won; Wurz, Ryan P; Achanta, Pragathi; Arvedson, Tara; Bartberger, Michael D; Campuzano, Iain D G; Fucini, Ray; Hansen, Stig K; Ingersoll, John; Iwig, Jeffrey S; Lipford, J Russell; Ma, Vu; Kopecky, David J; McCarter, John; San Miguel, Tisha; Mohr, Christopher; Sabet, Sudi; Saiki, Anne Y; Sawayama, Andrew; Sethofer, Steven; Tegley, Christopher M; Volak, Laurie P; Yang, Kevin; Lanman, Brian A; Erlanson, Daniel A; Cee, Victor J.
Affiliation
  • Shin Y; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Jeong JW; Carmot Therapeutics, Inc. 740 Heinz Avenue, Berkeley, California 94710, United States.
  • Wurz RP; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Achanta P; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Arvedson T; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Bartberger MD; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Campuzano IDG; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Fucini R; Carmot Therapeutics, Inc. 740 Heinz Avenue, Berkeley, California 94710, United States.
  • Hansen SK; Carmot Therapeutics, Inc. 740 Heinz Avenue, Berkeley, California 94710, United States.
  • Ingersoll J; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Iwig JS; Carmot Therapeutics, Inc. 740 Heinz Avenue, Berkeley, California 94710, United States.
  • Lipford JR; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Ma V; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Kopecky DJ; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • McCarter J; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • San Miguel T; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Mohr C; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Sabet S; Carmot Therapeutics, Inc. 740 Heinz Avenue, Berkeley, California 94710, United States.
  • Saiki AY; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Sawayama A; Carmot Therapeutics, Inc. 740 Heinz Avenue, Berkeley, California 94710, United States.
  • Sethofer S; Carmot Therapeutics, Inc. 740 Heinz Avenue, Berkeley, California 94710, United States.
  • Tegley CM; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Volak LP; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Yang K; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Lanman BA; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
  • Erlanson DA; Carmot Therapeutics, Inc. 740 Heinz Avenue, Berkeley, California 94710, United States.
  • Cee VJ; Departments of Therapeutic Discovery, Oncology Research, Pharmacokinetics and Drug Metabolism, Amgen Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.
ACS Med Chem Lett ; 10(9): 1302-1308, 2019 Sep 12.
Article in En | MEDLINE | ID: mdl-31531201