激肽释放酶
共晶
化学
小分子
立体化学
蛋白酶抑制剂(药理学)
组合化学
分子
生物化学
酶
有机化学
医学
氢键
人类免疫缺陷病毒(HIV)
抗逆转录病毒疗法
家庭医学
病毒载量
作者
Zhe Li,James R. Partridge,Abel Silva‐Garcia,Peter Rademacher,Andreas Betz,Qing Xu,Hing L. Sham,Yun‐Jin Hu,Yuqing Shan,Bin Liu,Ying Zhang,Haijuan Shi,Qiong Xu,Xubo Ma,Li Zhang
标识
DOI:10.1021/acsmedchemlett.6b00384
摘要
A series of macrocyclic analogues were designed and synthesized based on the cocrystal structure of small molecule plasma kallikrein (pKal) inhibitor, 2, with the pKal protease domain. This led to the discovery of a potent macrocyclic pKal inhibitor 29, with an IC50 of 2 nM for one olefinic isomer and 42.3 nM for the other olefinic isomer.
科研通智能强力驱动
Strongly Powered by AbleSci AI