广告
化学
兴奋剂
药理学
药物发现
药代动力学
糖尿病
临床试验
内科学
受体
生物化学
医学
内分泌学
作者
Lian Zhu Liu,Tianwei Ma,Jingye Zhou,Zhi Long Hu,Xue Zhang,Hai Zhen Zhang,Zeng Mi,Jia Liu,Lei Li,Yi Jiang,Zack Zou,Fan Wang,Lei Zhang,Jianfeng Xu,Sheng Wang,Fei Xiao,Xiankang Fang,Haixia Zou,Alexander M. Efanov,Melissa K. Thomas,Hua Lin,Jiehao Chen
标识
DOI：10.1016/j.bmcl.2019.126857
摘要
The discovery and optimization of a novel series of GPR142 agonists are described. These led to the identification of compound 21 (LY3325656), which demonstrated anti-diabetic benefits in pre-clinical studies and ADME/PK properties suitable for human dosing. Compound 21 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.
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