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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.
Humphreys, Philip G; Anderson, Niall A; Bamborough, Paul; Baxter, Andrew; Chung, Chun-Wa; Cookson, Rosa; Craggs, Peter D; Dalton, Toryn; Fournier, Julie C L; Gordon, Laurie J; Gray, Heather F; Gray, Matthew W; Gregory, Richard; Hirst, David J; Jamieson, Craig; Jones, Katherine L; Kessedjian, Hripsimee; Lugo, David; McGonagle, Grant; Patel, Vipulkumar K; Patten, Christopher; Poole, Darren L; Prinjha, Rab K; Ramirez-Molina, Cesar; Rioja, Inmaculada; Seal, Gail; Stafford, Kayleigh A J; Shah, Rishi R; Tape, Daniel; Theodoulou, Natalie H; Tomlinson, Laura; Ukuser, Sabri; Wall, Ian D; Wellaway, Natalie; White, Gemma.
Afiliação
  • Humphreys PG; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Anderson NA; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Bamborough P; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Baxter A; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Chung CW; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Cookson R; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Craggs PD; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Dalton T; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Fournier JCL; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Gordon LJ; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Gray HF; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Gray MW; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Gregory R; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Hirst DJ; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Jamieson C; WestCHEM, Department of Pure and Applied Chemistry, Thomas Graham Building, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, U.K.
  • Jones KL; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Kessedjian H; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Lugo D; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • McGonagle G; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Patel VK; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Patten C; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Poole DL; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Prinjha RK; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Ramirez-Molina C; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Rioja I; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Seal G; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Stafford KAJ; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Shah RR; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Tape D; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Theodoulou NH; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Tomlinson L; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Ukuser S; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Wall ID; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • Wellaway N; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
  • White G; GSK, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.
J Med Chem ; 65(22): 15174-15207, 2022 11 24.
Article em En | MEDLINE | ID: mdl-36378954
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Fatores de Transcrição / Lisina Tipo de estudo: Diagnostic_studies / Prognostic_studies Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Reino Unido
Texto completo
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Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Fatores de Transcrição / Lisina Tipo de estudo: Diagnostic_studies / Prognostic_studies Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Reino Unido