GPR3 inverse agonist-1

GPR3 inverse agonist-1 (compound 33) induces GPR3-specific conformational changes in stably transfected HEK293A cells, with an EC₅₀ of 5 μM, and exhibits selectivity for β₂AR^[1].
GPR3 inverse agonist-1 acts as a GPR3 inverse agonist in HEK293A cells expressing the G_s-CASE biosensor, and reduces basal G_s activity with an EC₅₀ of 250 nM^[1].
GPR3 inverse agonist-1 reduces basal cAMP levels in GPR3-expressing HEK293A cells with an EC₅₀ of 2 μM, and exhibits selectivity over the closely related GPR6 and GPR12 receptors^[1].
GPR3 inverse agonist-1 competes with the GPR3 agonist DPI for binding in HEK293A cells, but does not interfere with the binding of the inverse agonist AF64394, and exerts differential effects on the potencies of the endogenous agonists OEA and oleamide^[1].
At high concentrations, GPR3 inverse agonist-1 does not modulate agonist-induced signaling of A₂BR, CB₁R, S1PR1 or LPAR1 in HEK293A cells, indicating its selectivity for GPR3^[1].
GPR3 inverse agonist-1 retains its activity in HEK293A cells expressing GPR3 biosensor variants with extracellular loop 2 mutations, indicating that it has a distinct binding mode from rac-VH1/52^[1].
GPR3 inverse agonist-1 exhibits excellent physicochemical properties, including high synthetic accessibility and compliance with the Rule of Five, rendering it a lead structure suitable for further optimization^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.