Back to Search
Start Over
Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2020 Mar 01; Vol. 30 (5), pp. 126857. Date of Electronic Publication: 2019 Dec 27. - Publication Year :
- 2020
-
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.<br />Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2019 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Benzamides chemical synthesis
Benzamides pharmacokinetics
Dogs
Drug Discovery
Drug Evaluation, Preclinical
Gene Knockout Techniques
Humans
Hypoglycemic Agents chemical synthesis
Hypoglycemic Agents pharmacokinetics
Mice, Knockout
Molecular Structure
Rats
Receptors, G-Protein-Coupled genetics
Structure-Activity Relationship
Triazoles chemical synthesis
Triazoles pharmacokinetics
Benzamides therapeutic use
Diabetes Mellitus, Experimental drug therapy
Hypoglycemic Agents therapeutic use
Receptors, G-Protein-Coupled agonists
Triazoles therapeutic use
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 30
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 31982234
- Full Text :
- https://doi.org/10.1016/j.bmcl.2019.126857