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. 2020 Mar 2;9:e53779. doi: 10.7554/eLife.53779

Figure 3. Functional characterization of selected VLS hits for agonist activity at MT1 and MT2 receptors in Gi/o-mediated cAMP production inhibition assays.

Results were normalized to the Emax value (%) of receptor activation by melatonin. These VLS hits showed no activity at control HEK293 T cells without transiently transfected MT1 or MT2 receptors (results not shown).

Figure 3.

Figure 3—figure supplement 1. Radioligand 3H-Melatonin competition binding data for selected hit compounds.

Figure 3—figure supplement 1.

Results are normalized (mean ± SEM) from three independent assays, pooled and analyzed in GraphPad Prism 7.0.
Figure 3—figure supplement 2. Tango assay measuring agonist-induced β-arrestin recruitment by MT1receptor.

Figure 3—figure supplement 2.

Results were normalized to reference Melatonin (100%, mean ± SEM) from a minimum of three independent assays and pooled for analysis in GraphPad Prism 7.0.
Figure 3—figure supplement 3. Tango assay measuring agonist-induced β-arrestin recruitment by MT2receptor.

Figure 3—figure supplement 3.

Results were normalized to reference Melatonin (100%, mean ± SEM) from a minimum of three independent assays and pooled for analysis in GraphPad Prism 7.0.