Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19

Author:

Mallinger Aurélie1,Schiemann Kai2,Rink Christian1,Stieber Frank2,Calderini Michel2,Crumpler Simon1,Stubbs Mark1,Adeniji-Popoola Olajumoke1,Poeschke Oliver2,Busch Michael2,Czodrowski Paul2,Musil Djordje2,Schwarz Daniel2,Ortiz-Ruiz Maria-Jesus1,Schneider Richard2,Thai Ching1,Valenti Melanie1,de Haven Brandon Alexis1,Burke Rosemary1,Workman Paul1,Dale Trevor3,Wienke Dirk2,Clarke Paul A.1,Esdar Christina2,Raynaud Florence I.1,Eccles Suzanne A.1,Rohdich Felix2,Blagg Julian1

Affiliation:

1. Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, SW7 3RP, U.K.

2. Merck KGaA, Darmstadt, 64293, Germany

3. School of Bioscience, Cardiff University, Cardiff, CF10 3AX, U.K.

Funder

Cancer Research UK

Royal Marsden NHS Foundation Trust

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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