4 minute read
Jan. 28, 2023

A "Bow-Tie" Spirocyclopropyl LRRK2 Inhibitor from Merck

compound 25

kinome selective, CNS-penetrant, type I LRRK2 inhibitor in vivo activity in preclinical PK/PD model scaffold hopping + opt. of MLi-2 J. Med. Chem., December 7, 2022 Merck & Co., Boston, MA & Kenilworth, NJ

Drug Hunter Team

“Compound 25” is a selective, CNS-penetrant, ATP-competitive LRRK2 inhibitor that entered preclinical candidate enabling studies but was discontinued for undisclosed reasons. The molecule possesses two interesting chemical features: a “bow-tie” spirocyclopropyl group that made a significant impact on potency and overall properties, and a non-classical C-H hinge binder. The molecule was nominated by reviewer Dennis Koester, who says ...



Other molecules you may be interested in