Extended Data Fig. 1: Pharmacological assays to confirm signaling efficacy of small molecule ligands alvimopan, naloxone, mitragynineP, DAMGO and loperamide at human MOR.
From: Structural snapshots capture nucleotide release at the μ-opioid receptor
a, b, c ONE-GO, RG-BRET and TruPATH assay confirm relative signaling efficacy of alvimopan, naloxone, mitragynineP, DAMGO and loperamide. Data is a global fit of individual replicates. Data are plotted as raw netBRET ratios. d, cAMP inhibition assay (GloSensor) confirms relative signaling efficacy of alvimopan, naloxone, mitragynineP, DAMGO and loperamide. Data is a global fit of individual replicates. AU, arbitrary units. e, Homologous competition radioligand binding assay of [3H]naltrexone. Titration: concentration-dependent effects of GDPβS in the presence of 2 nM [3H]naltrexone. Data points are plotted as individual replicate values of raw netBRET ratios (a-c), luminescence (d), or specific binding (total binding minus nonspecific binding) (e), overlaid with nonlinear regression global fits. All plots are representative of three biologically independent experiments, with each data point carried out with three technical replicates.
