Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.

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Title: Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.
Authors: Humphreys PG; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Atkinson SJ; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Bamborough P; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Bit RA; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Chung CW; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Craggs PD; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Cutler L; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Davis R; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Ferrie A; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Gong G; WuXi Shanghai STA Pharmaceutical R&D Co., Ltd., No. 90 Delin Road, WaiGaoQiao Free Trade Zone, Shanghai 200131, China., Gordon LJ; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Gray M; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Harrison LA; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Hayhow TG; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Haynes A; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Henley N; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Hirst DJ; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Holyer ID; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Lindon MJ; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Lovatt C; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Lugo D; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., McCleary S; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Molnar J; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Osmani Q; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Patten C; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Preston A; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Rioja I; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Seal JT; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Smithers N; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Sun F; WuXi Shanghai STA Pharmaceutical R&D Co., Ltd., No. 90 Delin Road, WaiGaoQiao Free Trade Zone, Shanghai 200131, China., Tang D; WuXi Shanghai STA Pharmaceutical R&D Co., Ltd., No. 90 Delin Road, WaiGaoQiao Free Trade Zone, Shanghai 200131, China., Taylor S; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Theodoulou NH; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom.; WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde, Thomas Graham Building, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom., Thomas C; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Watson RJ; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Wellaway CR; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Zhu L; WuXi Shanghai STA Pharmaceutical R&D Co., Ltd., No. 90 Delin Road, WaiGaoQiao Free Trade Zone, Shanghai 200131, China., Tomkinson NCO; WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde, Thomas Graham Building, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom., Prinjha RK; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
Source: Journal of medicinal chemistry [J Med Chem] 2022 Feb 10; Vol. 65 (3), pp. 2262-2287. Date of Electronic Publication: 2022 Jan 07.
Publication Type: Journal Article; Research Support, Non-U.S. Gov't
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.1c01747