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

23 December 2019, Version 1

Abstract

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.

Keywords

Cyclin Dependent Kinases
CDK
cyclin
target engagement assay
selectivity
residence time
nanoBRET
BRET
energy transfer

Supplementary materials

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CDK Paper Supplement ChemRxiv 12182019
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