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

  • Bioorg Med Chem Lett. 2014 Nov 15;24(22):5195-8. doi: 10.1016/j.bmcl.2014.09.077.
Thomas Jensen  1 ,  Lisbeth Elster  1 ,  Søren Møller Nielsen  1 ,  Suresh Babu Poda  1 ,  Frosty Loechel  1 ,  Christiane Volbracht  1 ,  Ib Vestergaard Klewe  1 ,  Laurent David  1 ,  Stephen P Watson  1
Affiliations
  • 1. Neuroscience Drug Discovery, H-Lundbeck A/S, 2500 Valby, Copenhagen, Denmark.
PMID: 25442311 DOI: 10.1016/j.bmcl.2014.09.077
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.

Keywords
AF64394; G protein coupled receptor; GPR12; GPR3; GPR6; Inverse agonist; Orphan receptor.
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