Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human.


Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States. Electronic address: [Email]


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.


GPR142 agonist,Glucose-dependent insulin secretion,Metabolism,Type 2 diabetes,

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