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[Preprint]. 2024 Mar 13:2023.12.20.572662. Originally published 2023 Dec 21. [Version 2] doi: 10.1101/2023.12.20.572662

Extended Data Figure 10 |. Signaling profiles of the top functional hits against the 5-HT2A, 5-HT2B, and 5-HT2C receptors.

Extended Data Figure 10 |

a. Functional assays for the top agonists from the cryoEM docking campaign relative to 5-HT (open symbols and dotted lines). Calcium mobilization (top) against 5-HT2A (blue), 5-HT2B (red), and 5-HT2C (green) receptors. BRET assays (bottom) measuring Gαq protein dissociation (blue) or β-arrestin2 recruitment (red) at the 5-HT2A receptor. b. Functional assays for the top agonists from the AF2 docking campaign relative to 5-HT (open symbols and dotted lines). Calcium mobilization (top) against 5-HT2A (blue), 5-HT2B (red), and 5-HT2C (green) receptors. BRET assays (bottom) measuring Gαq protein dissociation (blue) or β-arrestin2 recruitment (red) at the 5-HT2A receptor. The chemical structure of each compound is displayed below its respective dose-response curve. c. BRET assays measuring Gαq protein dissociation (blue) or β-arrestin2 recruitment (red) for the top agonists from the cryoEM docking campaign for 5-HT2B (top) and 5-HT2C (bottom) receptors. d. BRET assays measuring Gαq protein dissociation (blue) or β-arrestin2 recruitment (red) for the top agonists from the AF2 docking campaign for 5-HT2B (top) and 5-HT2C (bottom) receptors. Data are normalized relative to 5-HT and presented as mean ± s.e.m. of three biological replicates.