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Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
Mallinger, Aurélie; Schiemann, Kai; Rink, Christian; Stieber, Frank; Calderini, Michel; Crumpler, Simon; Stubbs, Mark; Adeniji-Popoola, Olajumoke; Poeschke, Oliver; Busch, Michael; Czodrowski, Paul; Musil, Djordje; Schwarz, Daniel; Ortiz-Ruiz, Maria-Jesus; Schneider, Richard; Thai, Ching; Valenti, Melanie; de Haven Brandon, Alexis; Burke, Rosemary; Workman, Paul; Dale, Trevor; Wienke, Dirk; Clarke, Paul A; Esdar, Christina; Raynaud, Florence I; Eccles, Suzanne A; Rohdich, Felix; Blagg, Julian.
Affiliation
  • Mallinger A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Schiemann K; Merck KGaA , Darmstadt, 64293, Germany.
  • Rink C; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Stieber F; Merck KGaA , Darmstadt, 64293, Germany.
  • Calderini M; Merck KGaA , Darmstadt, 64293, Germany.
  • Crumpler S; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Stubbs M; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Adeniji-Popoola O; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Poeschke O; Merck KGaA , Darmstadt, 64293, Germany.
  • Busch M; Merck KGaA , Darmstadt, 64293, Germany.
  • Czodrowski P; Merck KGaA , Darmstadt, 64293, Germany.
  • Musil D; Merck KGaA , Darmstadt, 64293, Germany.
  • Schwarz D; Merck KGaA , Darmstadt, 64293, Germany.
  • Ortiz-Ruiz MJ; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Schneider R; Merck KGaA , Darmstadt, 64293, Germany.
  • Thai C; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Valenti M; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • de Haven Brandon A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Burke R; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Workman P; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Dale T; School of Bioscience, Cardiff University , Cardiff, CF10 3AX, U.K.
  • Wienke D; Merck KGaA , Darmstadt, 64293, Germany.
  • Clarke PA; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Esdar C; Merck KGaA , Darmstadt, 64293, Germany.
  • Raynaud FI; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Eccles SA; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
  • Rohdich F; Merck KGaA , Darmstadt, 64293, Germany.
  • Blagg J; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.
J Med Chem ; 59(3): 1078-101, 2016 Feb 11.
Article in En | MEDLINE | ID: mdl-26796641
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Cyclin-Dependent Kinases / Small Molecule Libraries / Drug Discovery / Cyclin-Dependent Kinase 8 / Aminopyridines Type of study: Risk_factors_studies Limits: Animals / Female / Humans / Male Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2016 Type: Article Affiliation country: United kingdom
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Cyclin-Dependent Kinases / Small Molecule Libraries / Drug Discovery / Cyclin-Dependent Kinase 8 / Aminopyridines Type of study: Risk_factors_studies Limits: Animals / Female / Humans / Male Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2016 Type: Article Affiliation country: United kingdom