Skip to main content
. Author manuscript; available in PMC: 2022 Dec 19.
Published in final edited form as: Nature. 2021 Dec 15;601(7893):452–459. doi: 10.1038/s41586-021-04220-9

Figure 4. Selection and characterization of the best analog series for CB2 hits from V-SYNTHES screening.

Figure 4.

(a) Chemical scaffold for the 523 antagonist analogs (b) Predicted binding poses of the best two analogs 733 and 747 in CB2 pocket. (c) Measured antagonist potencies and binding affinities for the best six analogs of 523. (d) Dose-response curves for the best six analogs tested in functional β-arrestin recruitment Tango assays at CB2, with SR144528 as a positive control. (e) Dose-response curves for the best six analogs at CB2 tested in radioligand binding assay, with compound AM10257 as a positive control. Both the Tango and binding assay data points are presented as mean ± SEM with n=3 independent experiments, each repeat carried out in triplicate.