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.
Bibliographical noteFunding Information:
*E-mail: email@example.com. *E-mail: firstname.lastname@example.org. ORCID William C. K. Pomerantz: 0000-0002-0163-4078 Ernst Schönbrunn: 0000-0002-3589-3510 Gunda I. Georg: 0000-0002-8900-9460 Jon E. Hawkinson: 0000-0001-5461-7071 Author Contributions ⊥These authors contributed equally. All authors have given approval to the final version of the manuscript. Funding Financial support for this project is gratefully acknowledged from the NICHD (HHSN27520130001 and 1 U54 HD09354) and NSF-CAREER Award CHE-1352091. Notes The authors declare no competing financial interest.
- bromodomain and extra-terminal domain
- fluorescence polarization
- pan-BET probe