化学
溴尿嘧啶
生物利用度
药理学
效力
生物化学
体外
医学
乙酰化
基因
作者
Changwei Wang,Mi Wang,Yu Wang,Rohan Kalyan Rej,Angelo Aguilar,Tianfeng Xu,Longchuan Bai,Jelena Tošović,Donna McEachern,Qiuxia Li,Farzad Sarkari,Bo Wen,Duxin Sun,Shaomeng Wang
标识
DOI:10.1021/acs.jmedchem.4c00971
摘要
The bromodomain-containing protein BRD9 has emerged as an attractive therapeutic target. In the present study, we successfully identified a number of highly potent BRD9 degraders by using two different cereblon ligands developed in our laboratory. Further optimization led to the discovery of CW-3308 as a potent, selective, and orally bioavailable BRD9 degrader. It displayed degradation potency (DC
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