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. 2013 Jun 1;23(11):3175-9.
doi: 10.1016/j.bmcl.2013.04.006. Epub 2013 Apr 10.

Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human

James S Scott  1 , Katy J Brocklehurst, Hayley S Brown, David S Clarke, Helen Coe, Sam D Groombridge, David Laber, Philip A MacFaul, Darren McKerrecher, Paul Schofield
Affiliations

Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human

James S Scott et al. Bioorg Med Chem Lett. .

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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