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submitted on 18.12.2019 and posted on 23.12.2019by 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.