Browsing by author "Eccles, Suzanne"
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A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Dale, T; Clarke, PA; Esdar, C; Waalboer, D; Adeniji-Popoola, O; et al. (NATURE PUBLISHING GROUP, 2015-12-01)There is unmet need for chemical tools to explore the role of the Mediator complex in human pathologies ranging from cancer to cardiovascular disease. Here we determine that CCT251545, a small-molecule inhibitor of the WNT ... -
The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.
Walton, MI; Eve, PD; Hayes, A; Henley, AT; Valenti, MR; et al. (IMPACT JOURNALS LLC, 2016-01-19)CCT245737 is the first orally active, clinical development candidate CHK1 inhibitor to be described. The IC50 was 1.4 nM against CHK1 enzyme and it exhibited>1,000-fold selectivity against CHK2 and CDK1. CCT245737 potently ...