Table 2. Binding Affinities and Functional Activity of the N-Boc-Protected DEG Probe Precursors.
Ki (nM) values obtained from [3H]CP55,940 displacement assays on CHO cell membranes stably expressing human CB1R or human CB2R. Values are means of three independent experiments performed in duplicate.
The activity levels (IC50) of 22b and 23b 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.
Maximum effect (Emax in %) was normalized to reference full agonist CP55,940. n.d. is not determined. All data with standard error of mean are given in the Supporting Information.