The identification of novel orally active mGluR5 antagonist GSK2210875

The identification of novel orally active mGluR5 antagonist GSK2210875 is described.

The identification of the novel orally active mGluR5 antagonist GSK2210875 is described. This MPEP competitive chemotype was identified via HTS and demonstrates intriguing and complex SAR distinct from known mGluR5 ligands. Notably a focus on polar compounds of modest potency but high free brain exposure afforded a compound with oral activity.Figure optionsDownload as PowerPoint slide