Abstract:
: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.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Paulson CN,Guan X,Ayoub AM,Chan A,Karim RM,Pomerantz WCK,Schönbrunn E,Georg GI,Hawkinson JEdoi
10.1021/acsmedchemlett.8b00380subject
Has Abstractpub_date
2018-10-31 00:00:00pages
1223-1229issue
12issn
1948-5875journal_volume
9pub_type
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