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Comprehensive Survey of CDK Inhibitor Selectivity in Live Cells with Energy Transfer Probes

submitted on 18.12.2019, 23:48 and posted on 23.12.2019, 20:27 by Carrow Wells, Jim Vasta, Cesear R. Corona, Jennifer Wilkinson, Chad A. Zimprich, Morgan R. Ingold, Julie E. Pickett, David Drewry, Kathryn Maria Pugh, Kilian Huber, Mei Cong, Poncho Meisenheimer, Timothy M. Willson, Matthew B. Robers
A panel of cell-permeable energy transfer probes has been developed to quantify target occupancy for all 21 CDKs in live, intact cells. Here we present the first comprehensive evaluation of intracellular isozyme potency and selectivity for a collection of 46 clinically-advanced CDKi’s and tool molecules. Here we provide a broadly applicable method for evaluating the selectivity of chemical matter for CDKs in living cells, and present a refined set of tool molecules to study CDK function.


Illuminating Function of the Understudied Druggable Kinome

National Institute of Diabetes and Digestive and Kidney Diseases

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A UK Hub to Catalyse Open Target Discovery.

Wellcome Trust

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Univerisity of North Carolina at Chapel Hill



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Declaration of Conflict of Interest

no conflict of interest