Discovery of GSK2656157: An optimized PERK inhibitor selected for preclinical development

ACS Medicinal Chemistry Letters

Volumn 4, Issue 10, 2013, Pages 964-968

  Axten, Jeffrey M ^a   Romeril, Stuart P ^a   Shu, Arthur ^a   Ralph, Jeffrey ^a   Medina, Jesús R ^a   Feng, Yanhong ^a   Li, William Hoi Hong ^a   Grant, Seth W ^a   Heerding, Dirk A ^a   Minthorn, Elisabeth ^a   Mencken, Thomas ^a   Gaul, Nathan ^a   Goetz, Aaron ^a   Stanley, Thomas ^a   Hassell, Annie M ^a   Gampe, Robert T ^a   Atkins, Charity ^a   Kumar, Rakesh ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

fluorine interaction; kinase; lead optimization; PERK; structure activity relationship; UPR

Indexed keywords

GSK 2656157; PROTEIN KINASE INHIBITOR; PROTEIN KINASE R; PROTEIN KINASE R LIKE ENDOPLASMIC RETICULUM KINASE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CANCER INHIBITION; CONTROLLED STUDY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG SCREENING; DRUG SELECTIVITY; ENDOPLASMIC RETICULUM; ENZYME ACTIVATION; HUMAN; HUMAN CELL; LIPOPHILICITY; LIVER MICROSOME; NONHUMAN; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; TUMOR XENOGRAFT;

MUS;

EID: 84885447174     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml400228e     Document Type: Article

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