Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377369 | Bioorganic & Medicinal Chemistry Letters | 2008 | 8 Pages |
Abstract
Ligand-based virtual screening led to the discovery of a new class of potent inverse agonists of the human cannabinoid receptor 1, hCB1, which are selective versus hCB2. These CB1 ligands present intriguing departures from a classical CB1 antagonist pharmacophore. Elements of SAR are discussed in this context.
Graphical abstracthCB1 antagonist pharmacophore → virtual screening → binding assay → functional assay → new class of potent hCB1 inverse agonists.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Nicolas Foloppe, Nicola H. Allen, Carol H. Bentley, Teresa D. Brooks, Guy Kennett, Antony R. Knight, Stefania Leonardi, Anil Misra, Nathaniel J.T. Monck, Daniel M. Sellwood,