The identification of GPR3 inverse agonist AF64394; The first small molecule inhibitor of GPR3 receptor function

The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported. [Display omitted] The identification of the novel and selective GP...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2014-11, Vol.24 (22), p.5195-5198
Main Authors: Jensen, Thomas, Elster, Lisbeth, Nielsen, Søren Møller, Poda, Suresh Babu, Loechel, Frosty, Volbracht, Christiane, Klewe, Ib Vestergaard, David, Laurent, Watson, Stephen P.
Format: Article
Language:English
Subjects:
AF64394
Animals
Drug Inverse Agonism
G protein coupled receptor
GPR12
GPR3
GPR6
Inverse agonist
Mice
Orphan receptor
Pyrimidines - chemistry
Pyrimidines - pharmacology
Receptors, G-Protein-Coupled - antagonists & inhibitors
Receptors, G-Protein-Coupled - physiology
Triazoles - chemistry
Triazoles - pharmacology
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Summary:The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported. [Display omitted] The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.09.077