Discovery of a potent class of PI3Kα inhibitors with unique binding mode via encoded library technology (ELT4)

ACS Medicinal Chemistry Letters

Volumn 6, Issue 5, 2015, Pages 531-536

  Yang, Hongfang ^a   Medeiros, Patricia F ^a   Raha, Kaushik ^b   Elkins, Patricia ^b   Lind, Kenneth E ^a   Lehr, Ruth ^b   Adams, Nicholas D ^a   Burgess, Joelle L ^a   Schmidt, Stanley J ^a   Knight, Steven D ^a   Auger, Kurt R ^a   Schaber, Michael D ^a   Franklin, G Joseph ^a   Ding, Yun ^a   Delorey, Jennifer L ^a,d   Centrella, Paolo A ^a,c   Mataruse, Sibongile ^a,d   Skinner, Steven R ^a   Clark, Matthew A ^a,c   Cuozzo, John W ^a,c   Evindar, Ghotas ^a   more..

^a GLAXOSMITHKLINE   (United States)

^b Computational and Structural Chemistry Platform Technology and Science Platform Technology and Science ^*  (United States)

^c X Chem Incorporated   (United States)

^d MASSACHUSETTS COLLEGE OF PHARMACY AND HEALTH SCIENCES   (United States)

Author keywords

ELT; Encoded Library technology; p110 ; PI3K p110 (H1047R); PI3K

Indexed keywords

2 (2 DIFLUOROMETHYLBENZIMIDAZOL 1 YL) 4,6 DIMORPHOLINO 1,3,5 TRIAZINE; ADENOSINE TRIPHOSPHATE; ALDEHYDE; ANILINE; CARBONYL DERIVATIVE; CARBOXYLIC ACID; P110 ALPHA PROTEIN; PHOSPHATIDYLINOSITOL 3 KINASE ALPHA INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PHOSPHOTRANSFERASE INHIBITOR; PROTEIN P110; SULFONAMIDE; UNCLASSIFIED DRUG;

AMINATION; ARTICLE; BINDING SITE; COMPETITIVE INHIBITION; CRYSTAL STRUCTURE; DNA LIBRARY; DNA SYNTHESIS; ENCODED LIBRARY TECHNOLOGY; ENZYME ACTIVE SITE; HYDROGEN BOND; METHYLATION; PHARMACOPHORE; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; STATIC ELECTRICITY; SUZUKI REACTION; SYNTHESIS; WILD TYPE;

EID: 84929315987     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.5b00025     Document Type: Article

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