Chemical Information

Biological Activity of GNE-9605

GNE-9605 is a highly potent, selective, and brain-penetrant LRRK2 inhibitor with IC50 of 19 nM.
IC50 value:
Target: LRRK2
GNE-9605 retained excellent predicted human metabolic stability when assayed in human liver microsomes and hepatocytes. In addition, no reversible or time-dependent inhibition of any of the major CYP isoforms was observed. The demonstrated metabolic stability, brain penetration across multiple species, and selectivity of these inhibitors support their use in preclinical efficacy and safety studies.

References on GNE-9605

[1]. Estrada AA, et al. Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem. 2014 Feb 13;57(3):921-36.