Extended Data Fig. 7: Screening and signal profiling of GPR101 agonists.
From: Structure of GPR101–Gs enables identification of ligands with rejuvenating potential
a, An overview of the algorithm for in silico GPR101 ligands screening and validation. b, The docking scores of the 137 candidate compounds revealed by DOCK4.025. c, Summarized EC50 and Emax values of different ligands in activating Gs, Gq or β-arrestin2 pathways downstream of GPR101. AA-1 was used as the negative control. Values represent the mean ± SEM from three independent experiments (n = 3) performed in triplicate. ND, not detectable. d, Summarized biased factors and bias properties of the GPR101 agonists. β values (bias factor) of the selective ligands towards individual pathway were calculated using AA-14-induced Gq activation as the reference. Data are from three independent experiments (n = 3) performed in triplicates.
