Despite the poor pharmacokinetic properties, 5 was used to demonstrate that selective BD1 inhibitors may be equally effective as pan‐BET inhibitors in cancer cells.[7] Compound 6 showed a 1000‐fold selectivity for BD1 over BD2 in all BET proteins with an inhibition in the low nanomolar range (IC50=30 nM). The gene discussed is DNER; the disease is cancer.