首页> Journal of medicinal chemistry> Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.

Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.

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第一作者： Philip G,Humphreys

第一单位： GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.

作者： Philip G,Humphreys ^[1] ; Niall A,Anderson ^[1] ; Paul,Bamborough ^[1] ; Andrew,Baxter ^[1] ; Chun-Wa,Chung ^[1] ; Rosa,Cookson ^[1] ; Peter D,Craggs ^[1] ; Toryn,Dalton ^[1] ; Julie C L,Fournier ^[1] ; Laurie J,Gordon ^[1] ; Heather F,Gray ^[1] ; Matthew W,Gray ^[1] ; Richard,Gregory ^[1] ; David J,Hirst ^[1] ; Craig,Jamieson ^[2] ; Katherine L,Jones ^[1] ; Hripsimee,Kessedjian ^[1] ; David,Lugo ^[1] ; Grant,McGonagle ^[1] ; Vipulkumar K,Patel ^[1] ; Christopher,Patten ^[1] ; Darren L,Poole ^[1] ; Rab K,Prinjha ^[1] ; Cesar,Ramirez-Molina ^[1] ; Inmaculada,Rioja ^[1] ; Gail,Seal ^[1] ; Kayleigh A J,Stafford ^[1] ; Rishi R,Shah ^[1] ; Daniel,Tape ^[1] ; Natalie H,Theodoulou ^[1] ; Laura,Tomlinson ^[1] ; Sabri,Ukuser ^[1] ; Ian D,Wall ^[1] ; Natalie,Wellaway ^[1] ; Gemma,White ^[1]

作者单位： GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K. ^[1] WestCHEM, Department of Pure and Applied Chemistry, Thomas Graham Building, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, U.K. ^[2]

医学主题词人类(Humans);赖氨酸(Lysine);配体(Ligands);转录因子(Transcription Factors);组蛋白类(Histones)

DOI 10.1021/acs.jmedchem.2c01102

PMID 36378954

发布时间 2022-12-20

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