Article
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
Bioorganic & medicinal chemistry letters - 1 Mar 2012
Zhang Jinwei, Deng Xianming, Choi Hwan Geun, Alessi Dario R, Gray Nathanael S
Abstract excerpt
Leucine-rich repeat kinase 2 (LRRK2) is linked to Parkinson's disease and may represent an attractive therapeutic target. Here we report a 2,4-dianilino-5-chloro-pyrimidine, TAE684, a previously reported inhibitor of anaplastic lymphoma kinase (ALK), is also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant). TAE684 substantially inhibits Ser910...
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