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Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-12-27 , DOI: 10.1016/j.bmcl.2019.126857 Lian Zhu Liu 1 , Tianwei Ma 2 , Jingye Zhou 2 , Zhi Long Hu 2 , Xue Jun Zhang 2 , Hai Zhen Zhang 2 , Mi Zeng 2 , Jia Liu 2 , Lei Li 2 , Yi Jiang 2 , Zack Zou 2 , Fan Wang 2 , Lei Zhang 2 , Jianfeng Xu 2 , Jingru Wang 2 , Fei Xiao 2 , Xiankang Fang 2 , Haixia Zou 1 , Alexander M Efanov 3 , Melissa K Thomas 3 , Hua V Lin 2 , Jiehao Chen 3
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-12-27 , DOI: 10.1016/j.bmcl.2019.126857 Lian Zhu Liu 1 , Tianwei Ma 2 , Jingye Zhou 2 , Zhi Long Hu 2 , Xue Jun Zhang 2 , Hai Zhen Zhang 2 , Mi Zeng 2 , Jia Liu 2 , Lei Li 2 , Yi Jiang 2 , Zack Zou 2 , Fan Wang 2 , Lei Zhang 2 , Jianfeng Xu 2 , Jingru Wang 2 , Fei Xiao 2 , Xiankang Fang 2 , Haixia Zou 1 , Alexander M Efanov 3 , Melissa K Thomas 3 , Hua V Lin 2 , Jiehao Chen 3
Affiliation
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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.
中文翻译：
LY3325656的发现：适用于人类临床测试的GPR142激动剂。
描述了新型GPR142激动剂的发现和优化。这些导致了化合物21（LY3325656）的鉴定，该化合物在临床前研究中显示出抗糖尿病的益处以及适用于人类给药的ADME / PK特性。化合物21是第一个进入1期临床试验以治疗2型糖尿病的GPR142激动剂分子。
更新日期：2019-12-27
中文翻译：
LY3325656的发现：适用于人类临床测试的GPR142激动剂。
描述了新型GPR142激动剂的发现和优化。这些导致了化合物21（LY3325656）的鉴定，该化合物在临床前研究中显示出抗糖尿病的益处以及适用于人类给药的ADME / PK特性。化合物21是第一个进入1期临床试验以治疗2型糖尿病的GPR142激动剂分子。
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