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Based on a previously reported 1,4‐dihydropyridinebutyrolactone virtual screening hit, nine lactone ring‐opened ester and seven amide analogs were prepared. The analogs were designed to provide interactions with residues at the entrance of the ZA loop of the testis‐specific bromodomain (ZA) channel to enhance the affinity and selectivity for the bromodomain and extra‐terminal (BET) subfamily of bromodomains...