Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library

ACS Medicinal Chemistry Letters

Volumn 6, Issue 8, 2015, Pages 919-924

  Deng, Hongfeng ^a   Zhou, Jingye ^a,e   Sundersingh, Flora S ^a   Summerfield, Jennifer ^a   Somers, Don ^b   Messer, Jeffrey A ^a   Satz, Alexander L ^a,f   Ancellin, Nicolas ^c   Arico Muendel, Christopher C ^a   Bedard, Katie L ^a   Beljean, Arthur ^b   Belyanskaya, Svetlana L ^a   Bingham, Ryan ^b   Smith, Sarah E ^b   Boursier, Eric ^c   Carter, Paul ^b   Centrella, Paolo A ^a,g   Clark, Matthew A ^a,g   Chung, Chun Wa ^b   Davie, Christopher P ^a   Delorey, Jennifer L ^a   Ding, Yun ^a   Franklin, G Joseph ^a   Grady, LaShadric C ^a   Herry, Kenny ^c   Hobbs, Clare ^b   Kollmann, Christopher S ^a   Morgan, Barry A ^a   Kaushansky, Laura J ^a,h   Zhou, Quan ^d,i   more..

^a GLAXOSMITHKLINE   (United States)

^b GLAXOSMITHKLINE   (United Kingdom)

^c GLAXOSMITHKLINE   (France)

^d BRANDEIS UNIVERSITY   (United States)

^e ELI LILLY AND COMPANY   (United States)

^f F HOFFMANN LA ROCHE LTD   (Switzerland)

^g X Chem Incorporated   (United States)

^h UNIVERSITY OF MASSACHUSETTS MEDICAL SCHOOL   (United States)

ⁱ ASTRAZENECA   (United Kingdom)

Author keywords

BCATm; DNA Encoded Library; ELT; obesity; on DNA Suzuki Miyaura cross coupling reaction

Indexed keywords

3 [[ 1 ( 5 BROMOTHIOPHENE 2 CARBONYL)PYRROLIDIN 3 YL]OXY] N METHYL 2' (METHYLSULFONAMIDO)[ 1,1' BIPHENYL] 4 CARBOXAMIDE; AMINOTRANSFERASE; AMINOTRANSFERASE INHIBITOR; DNA; MITOCHONDRIAL BRANCHED CHAIN AMINOTRANSFERASE; MITOCHONDRIAL BRANCHED CHAIN AMINOTRANSFERASE INHIBITOR; PROTEOLIPID PROTEIN; PYRROLIDINE DERIVATIVE; THIOPHENE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CATALYSIS; CRYSTAL STRUCTURE; DNA LIBRARY; DNA SYNTHESIS; DRUG DESIGN; DRUG DETERMINATION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; IC50; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEIN STRUCTURE; STRUCTURE ACTIVITY RELATION; SUZUKI REACTION; X RAY CRYSTALLOGRAPHY;

EID: 84938911306     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.5b00179     Document Type: Article

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