Figure 3: Heatmap of ΔΔlogR values resulting from the operational analysis.
From: Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity
The operational analysis was performed using the procedure described in the Supplementary Information, with data obtained from three independent experiments performed in duplicate. Dark blue indicates bias towards the first pathway, while dark red indicates bias towards the second pathway. White boxes are not determined. (a) The operational analysis on hCB2R was done with all agonists, except HU210, which was tested in only two functional assays due to legal restrictions. Because of error propagation in the analysis, only a few were found to be statistically significant (P<0.05). (b) The operational analysis on mCB2R was done with the three most selective and most broadly active compounds on hCB2R; HU308, HU910 and JWH133. Here, all three ligands showed statistically significant bias towards G-protein signalling. Statistics was performed with one-way ANOVA Holm-Sidak’s multiple comparisons test using Graphpad Prism 6.
