image adapted from https://next.cancer.gov/discoveryResources/cbc.htm, Division of Cancer Treatment and Diagnosis, National Cancer Institute, part of the U.S. National Institutes of Health’
IRBM’s drug discovery research is featured on the cover of this issue’s ACS Publications’ Medicinal Chemistry Letters
The publication describes the discovery of a novel series of Imidazopyrazine derivatives by IRBM’s drug discovery team. This novel series of SHP2 allosteric inhibitors, having an imidazopyrazine 6,5-fused heterocyclic system as central scaffold, showed an excellent potency in enzyme and cellular assays. X-ray studies confirmed novel stabilizing interactions with respect to known SHP2 inhibitors. These compounds paved the way to the discovery of preclinical candidates.