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Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Sperandio, David; Aktoudianakis, Vangelis; Babaoglu, Kerim; Chen, Xiaowu; Elbel, Kristyna; Chin, Gregory; Corkey, Britton; Du, Jinfa; Jiang, Bob; Kobayashi, Tetsuya; Mackman, Richard; Martinez, Ruben; Yang, Hai; Zablocki, Jeff; Kusam, Saritha; Jordan, Kim; Webb, Heather; Bates, Jamie G; Lad, Latesh; Mish, Michael; Niedziela-Majka, Anita; Metobo, Sammy; Sapre, Annapurna; Hung, Magdeleine; Jin, Debi; Fung, Wanchi; Kan, Elaine; Eisenberg, Gene; Larson, Nate; Newby, Zachary E R; Lansdon, Eric; Tay, Chin; Neve, Richard M; Shevick, Sophia L; Breckenridge, David G.
Affiliation
  • Sperandio D; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA. Electronic address: david.sperandio@r2mpharma.com.
  • Aktoudianakis V; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Babaoglu K; Department of Structural Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Chen X; Department of Structural Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Elbel K; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Chin G; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Corkey B; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Du J; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Jiang B; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Kobayashi T; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Mackman R; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Martinez R; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Yang H; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Zablocki J; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Kusam S; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Jordan K; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Webb H; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Bates JG; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Lad L; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Mish M; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Niedziela-Majka A; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Metobo S; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Sapre A; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Hung M; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Jin D; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Fung W; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Kan E; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Eisenberg G; Department of Drug Metabolism, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Larson N; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Newby ZER; Department of Structural Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Lansdon E; Department of Structural Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Tay C; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Neve RM; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Shevick SL; Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
  • Breckenridge DG; Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
Bioorg Med Chem ; 27(3): 457-469, 2019 02 01.
Article de En | MEDLINE | ID: mdl-30606676
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Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Sujet principal: Facteurs de transcription / Benzimidazoles / Découverte de médicament / Isoxazoles / Myélome multiple Type d'étude: Prognostic_studies Limites: Animals / Humans Langue: En Journal: Bioorg Med Chem Sujet du journal: BIOQUIMICA / QUIMICA Année: 2019 Type de document: Article Pays de publication: Royaume-Uni
Texte intégral
Ajouter à My VHL
Imprimer
XML
PubMed Links
Recherche sur Google

Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Sujet principal: Facteurs de transcription / Benzimidazoles / Découverte de médicament / Isoxazoles / Myélome multiple Type d'étude: Prognostic_studies Limites: Animals / Humans Langue: En Journal: Bioorg Med Chem Sujet du journal: BIOQUIMICA / QUIMICA Année: 2019 Type de document: Article Pays de publication: Royaume-Uni