Several chemical probes have been developed for use in fluorescence polarization screening assays to aid in drug discovery for the bromodomain and extra-terminal domain (BET) proteins. However, few of those have been characterized in the literature. We have designed, synthesized, and thoroughly characterized a novel fluorescence polarization pan-BET chemical probe suitable for high-throughput screening, structure-activity relationships, and hit-to-lead potency and selectivity assays to identify and characterize BET bromodomain inhibitors.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6295860 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.8b00380 | DOI Listing |
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