BRD4 and cancer: The compounds are potent (Kd in the 10-9–10-8 M range), highly selective (>1000-fold) against BRD4-BD1 and a panel of kinase and GPCR targets, have acceptable ADME and PK profiles, block AML cancer cell proliferation at ~1 μM and display efficacious antitumor activity in a xenograft model of human AML [79], providing the most high-quality chemical probes for BRD7/9 described to date.