Table 1. Binding Affinities and Functional Activity of CB₁R DEG Ligands.

^aK_i (nM) values obtained from [³H]CP55,940 displacement assays on CHO membranes stably expressing human CB₁R or human CB₂R. Values are means of three independent experiments performed in duplicate.

^bThe activity levels (EC₅₀ or IC₅₀) of 14–19 were measured using cells stably expressing hCB₁R in homogeneous time-resolved fluorescence (HTRF) cAMP assay. The data are the means of three independent experiments performed in technical replicates.

^cMaximum effect (E_max in %) was normalized to reference full agonist CP55,940. n.a. denotes no activity. All data with standard error of mean are given in the Supporting Information.