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. 2020 Mar 11;63(7):3701–3712. doi: 10.1021/acs.jmedchem.0c00012

Figure 1.

Figure 1

PXR agonist activity and binding properties of GA. Binding activity of GA (1) was assessed by the AlphaScreen test at 10 μM compound concentration (A) and during a dose-dependent experiment (B). Comparisons were made with a series of vitamin E compounds and the PXR agonist 0.05 μM T0901317 (see Table S1). Calorimetric titrations of GA binding to PXR-LBD (C) were investigated in comparison with compounds 2 and 5 dissolved in DMSO and then further diluted to 60 μM final concentration in 25 mM Hepes buffer, pH 7.5, containing 150 mM NaCl. The final concentration of PXR-LBD in the reaction mixture was 3 μM, and DMSO was 8% v/v.