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Updated: May 16, 2026

Assaying the Kinase Activity of LRRK2 in vitro
Published on: January 18, 2012
Novel cinnoline-based inhibitors of LRRK2 kinase activity
Albert W Garofalo1, Marc Adler, Danielle L Aubele
1Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Blvd, South San Francisco, CA 94080, United States. albert.garofalo@elan.com
Abstract:
Leucine rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson's disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic approach that may lead to new treatments for PD. Herein we report the discovery of a series of cinnoline-3-carboxamides that are potent against both wild-type and mutant LRRK2 kinase activity in biochemical assays. These compounds are also shown to be potent inhibitors in a cellular assay and to have good to excellent CNS penetration.
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