Title : Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor.

Pub. Date : 2017 Sep 8

PMID : 28586718






1 Functional Relationships(s)
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1 Interestingly, some kinase inhibitors have been demonstrated to be potent bromodomain inhibitors, especially the PLK1 inhibitor BI-2536 and the JAK2 inhibitor TG101209, which can bind to BRD4 with IC50 values of 0.025 muM and 0.13 muM, respectively. BI 2536 bromodomain containing 4 Homo sapiens