CID-1375606 is a GPR27 agonist with EC50 values of 0.46 ?M and 7.9 ?M in chimeric GPR27V2 and wild-type GPR27 luciferase β-arrestin-2 complementation assays, respectively.1 It is selective for GPR27 over the closely related receptors GPR85 and GPR173 for which it does not induce β-arrestin-2 recruitment in the same assay. GPR27 function has been linked to insulin promoter activity and excretion.2
1.Dupuis, N., Laschet, C., Franssen, D., et al.Activation of the orphan G protein-coupled receptor GPR27 by surrogate ligands promotes β-arrestin 2 recruitmentMol. Pharmacol.91(6)595-608(2017) 2.Ku, G.M., Pappalardo, Z., Luo, C.C., et al.An siRNA screen in pancreatic beta cells reveals a role for Gpr27 in insulin productionPLoS Genet.8(1)e1002449(2012)