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Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human.
Liu, Lian Zhu; Ma, Tianwei; Zhou, Jingye; Long Hu, Zhi; Jun Zhang, Xue; Zhen Zhang, Hai; Zeng, Mi; Liu, Jia; Li, Lei; Jiang, Yi; Zou, Zack; Wang, Fan; Zhang, Lei; Xu, Jianfeng; Wang, Jingru; Xiao, Fei; Fang, Xiankang; Zou, Haixia; Efanov, Alexander M; Thomas, Melissa K; Lin, Hua V; Chen, Jiehao.
Afiliación
  • Liu LZ; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China; Lilly China Innovation and Partnerships (LCIP), Eli Lilly & Company, 16F, Tower1 HKRI, Taikoo Hui 288 Shimenyi Road, Shanghai 200041, PR China.
  • Ma T; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Zhou J; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Long Hu Z; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Jun Zhang X; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Zhen Zhang H; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Zeng M; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Liu J; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Li L; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Jiang Y; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Zou Z; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Wang F; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Zhang L; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Xu J; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Wang J; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Xiao F; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Fang X; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Zou H; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China; Lilly China Innovation and Partnerships (LCIP), Eli Lilly & Company, 16F, Tower1 HKRI, Taikoo Hui 288 Shimenyi Road, Shanghai 200041, PR China.
  • Efanov AM; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
  • Thomas MK; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
  • Lin HV; Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
  • Chen J; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States. Electronic address: chen_jiehao@lilly.com.
Bioorg Med Chem Lett ; 30(5): 126857, 2020 03 01.
Article en En | MEDLINE | ID: mdl-31982234
ABSTRACT
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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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Triazoles / Benzamidas / Receptores Acoplados a Proteínas G / Diabetes Mellitus Experimental / Hipoglucemiantes Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article
Texto completo
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Triazoles / Benzamidas / Receptores Acoplados a Proteínas G / Diabetes Mellitus Experimental / Hipoglucemiantes Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article