The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits

Author:

Bertrand Sophie M.12,Ancellin Nicolas3,Beaufils Benjamin3,Bingham Ryan P.1,Borthwick Jennifer A.12,Boullay Anne-Bénédicte3,Boursier Eric3,Carter Paul S.1,Chung Chun-wa1,Churcher Ian1,Dodic Nerina3,Fouchet Marie-Hélène3,Fournier Charlène1,Francis Peter L.1,Gummer Laura A.1,Herry Kenny3,Hobbs Andrew1,Hobbs Clare I.1,Homes Paul1,Jamieson Craig2,Nicodeme Edwige3,Pickett Stephen D.1,Reid Iain H.1,Simpson Graham L.1,Sloan Lisa A.1,Smith Sarah E.1,Somers Donald O’N.1,Spitzfaden Claus1,Suckling Colin J.2,Valko Klara1,Washio Yoshiaki1,Young Robert J.1

Affiliation:

1. GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

2. Department of Pure and Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow, G1 1XL, U.K.

3. Centre de Recherche, GlaxoSmithKline R&D, Les Ulis, 25, 27 Avenue du Québec, 91140 Villebon sur Yvette, France

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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