Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 21, 2015, Pages 4728-4732

  Burdick, Daniel J ^a   Wang, Shumei ^a   Heise, Christopher ^a   Pan, Borlan ^a   Drummond, Jake ^a   Yin, Jianping ^a   Goeser, Lauren ^a   Magnuson, Steven ^a   Blaney, Jeff ^a   Moffat, John ^a   Wang, Weiru ^a   Chen, Huifen ^a  

^a GENENTECH INC   (United States)

Author keywords

ERK2; Extracellular regulated kinase; Fragment based; Pyrrolopyrazine

Indexed keywords

5H PYRROLO[3,2 B]PYRAZINE DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; N BENZYL 9H PURIN 6 AMINE; PYRAZINE DERIVATIVE; PYRROLOPYRAZINE INHIBITOR; UNCLASSIFIED DRUG; MAPK1 PROTEIN, HUMAN; PYRROLE DERIVATIVE;

ARTICLE; CRYSTAL STRUCTURE; DRUG BINDING; DRUG POTENCY; DRUG SCREENING; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DEVELOPMENT; HUMAN; METABOLISM; SYNTHESIS;

DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HUMANS; MITOGEN-ACTIVATED PROTEIN KINASE 1; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PYRAZINES; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84944161005     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.08.048     Document Type: Article

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