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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| Published in | Bioorganic & medicinal chemistry letters Vol. 24; no. 22; pp. 5195 - 5198 |
|---|---|
| Main Authors | , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
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Elsevier Ltd
15.11.2014
Elsevier |
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| Abstract | 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. |
|---|---|
| AbstractList | 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. 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. 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. (C) 2014 Elsevier Ltd. All rights reserved. |
| Author | Jensen, Thomas Klewe, Ib Vestergaard Nielsen, Søren Møller Poda, Suresh Babu Elster, Lisbeth Watson, Stephen P. Loechel, Frosty David, Laurent Volbracht, Christiane |
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| Cites_doi | 10.1021/jm900319e 10.1016/j.neuropharm.2011.02.014 10.1021/jm200265b 10.1371/journal.pone.0074680 10.1038/nm.3023 10.1124/jpet.114.213082 10.1371/journal.pone.0004704 10.1111/j.1476-5381.2012.02043.x 10.1074/jbc.M700911200 10.1002/cber.19711040908 10.1016/S1359-6446(05)03386-6 10.1515/znb-1999-0614 10.1186/gb-2002-3-11-research0063 10.1016/S0898-6568(02)00041-4 |
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| Keywords | AF64394 GPR12 G protein coupled receptor Inverse agonist GPR3 GPR6 Orphan receptor LIGAND |
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| SubjectTerms | AF64394 Animals Chemistry Chemistry, Medicinal Chemistry, Organic Drug Inverse Agonism G protein coupled receptor GPR12 GPR3 GPR6 Inverse agonist Life Sciences & Biomedicine Mice Orphan receptor Pharmacology & Pharmacy Physical Sciences Pyrimidines - chemistry Pyrimidines - pharmacology Receptors, G-Protein-Coupled - antagonists & inhibitors Receptors, G-Protein-Coupled - physiology Science & Technology Triazoles - chemistry Triazoles - pharmacology |
| Title | The identification of GPR3 inverse agonist AF64394; The first small molecule inhibitor of GPR3 receptor function |
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