| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373432 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
The identification of novel orally active mGluR5 antagonist GSK2210875 is described.
Graphical abstractThe 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 full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Maria Pilla, Michela Andreoli, Michela Tessari, Sonia Delle-Fratte, Adelheid Roth, Sharon Butler, Fiona Brown, Parita Shah, Ezio Bettini, Palmina Cavallini, Roberto Benedetti, Doug Minick, Paul Smith, Ben Tehan, Pier D’Alessandro, Olivier Lorthioir,