Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369140 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
A series of conformationally restricted GPR119 agonists were prepared based around a 3,8-diazabicyclo[3.2.1]octane scaffold. Examples were found to have markedly different pharmacology in mouse and human despite similar levels of binding to the receptor. This highlights the large effects on GPCR phamacology that can result from small structural changes in the ligand, together with inter-species differences between receptors.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
James S. Scott, Katy J. Brocklehurst, Hayley S. Brown, David S. Clarke, Helen Coe, Sam D. Groombridge, David Laber, Philip A. MacFaul, Darren McKerrecher, Paul Schofield,