[14] were the first to characterize a thieno-triazolo-1,4-diazepine histone-binding module inhibitor, JQ1, a cell-permeable small molecule that competitively and specifically binds to the BD1 and BD2 bromodomains with high affinity; this then paved the way for the further development of other BET inhibitors, now being assessed clinically across a range of cancers. Here, DNER is linked to cancer.