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GSK2578215A: a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor

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  • Alastair D. Reith
  • Paul Bamborough
  • Karamjit Jandu
  • Daniele Andreotti
  • Lucy Mensah
  • Pamela Dossang
  • Hwan Geun Choi
  • Xianming Deng
  • Jinwei Zhang
  • Dario R. Alessi
  • Nathanael S. Gray

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Original languageEnglish
Pages (from-to)5625-5629
Number of pages5
JournalBioorganic & Medicinal Chemistry Letters
Issue number17
StatePublished - 2012


Leucine-rich repeat kinase 2 (LRRK2) is a promising therapeutic target for some forms of Parkinson's disease. Here we report the discovery and characterization of 2-arylmethyloxy-5-subtitutent-N-arylbenzamides with potent LRRK2 activities exemplified by GSK2578215A which exhibits biochemical IC s of around 10 nM against both wild-type LRRK2 and the G2019S mutant. GSK2578215A exhibits exceptionally high selectivity for LRRK2 across the kinome, substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.3-1.0 µM in cells and in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg.



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