The BMS BET inhibitor, BMS-986158 , is in a Ph. I/IIa trial in advanced cancers. During the optimization of the molecule from a carbazole hit, the authors employed a bold scaffold-hopping strategy involving changing the direction of the carbazole core in order to better access a hydrophobic region of the target. The proposed new binding mode [...]
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Nov. 26, 2021
BMS-986158: A BET Inhibitor
BMS-986158
oral BET inhibitor 4.5 mg QD, phase I/II for cancer from bromodomain-focused HTS, SBDD Journal of Medicinal Chemistry Bristol Myers Squibb