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Bioorganic and Medicinal Chemistry Letters

Volumn 26, Issue 5, 2016, Pages 1443-1451

Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore

(15) Schiemann, Kai a Mallinger, Aurélie b Wienke, Dirk a Esdar, Christina a Poeschke, Oliver a Busch, Michael a Rohdich, Felix a Eccles, Suzanne A b Schneider, Richard a Raynaud, Florence I b Czodrowski, Paul a Musil, Djordje a Schwarz, Daniel a Urbahns, Klaus a Blagg, Julian b

a MERCK KGAA (Germany)

b INSTITUTE OF CANCER RESEARCH (United Kingdom)

Author keywords

CDK19; CDK8; HSP90; Indazoles; Mediator complex; WNT pathway inhibitors

Indexed keywords

3 BENZYLINDAZOLE DERIVATIVE; ADENOSINE TRIPHOSPHATE; BIOLOGICAL MARKER; CYCLIN DEPENDENT KINASE 19; CYCLIN DEPENDENT KINASE 8; CYCLIN DEPENDENT KINASE 8 INHIBITOR; CYCLIN DEPENDENT KINASE INHIBITOR; HEAT SHOCK PROTEIN 90; STAT1 PROTEIN; UNCLASSIFIED DRUG; WNT PROTEIN; CDK8 PROTEIN, HUMAN; INDAZOLE DERIVATIVE; PROTEIN KINASE INHIBITOR;

ARTICLE; BINDING AFFINITY; CANCER MODEL; CRYSTAL STRUCTURE; DRUG BINDING SITE; DRUG POTENCY; DRUG SELECTIVITY; HIGH THROUGHPUT SCREENING; HUMAN; NONHUMAN; PHARMACOPHORE; PHYSICOCHEMICAL MODEL; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT; X RAY CRYSTALLOGRAPHY; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; COLORECTAL NEOPLASMS; DOSE RESPONSE; DRUG DEVELOPMENT; ENZYME SPECIFICITY; METABOLISM; MOLECULAR MODEL; MOUSE; RAT;

ANIMALS; COLORECTAL NEOPLASMS; CRYSTALLOGRAPHY, X-RAY; CYCLIN-DEPENDENT KINASE 8; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HSP90 HEAT-SHOCK PROTEINS; HUMANS; INDAZOLES; MICE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 84957850970 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2016.01.062 Document Type: Article

Times cited : (34)

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