Recently, Professor Xie Yusheng from the School of Basic Medical Sciences, Shandong University, in collaboration with Professor Yao Shaoqin from the National University of Singapore, Professor Wang Rui from the Shenzhen Bay Laboratory, and Professor Zhang Zhimin from Jinan University, published an online research paper entitled “Lysine-targeting, Covalent Inhibitors of Bromodomain BD1 of BET Proteins in Live Cells and Animals” in Angewandte Chemie International Edition. Based on the systematic mapping of the ligandability landscape of lysines in BRDs in live cells and animals, this study designed and developed BDS4/BDS6, the first selective covalent inhibitor of BET-BD1.