Figure 1. Cell-based qHTS assay optimization and hCAR agonist identification.

A double stable cell line, HepG2-CYP2B6-hCAR, was generated and utilized to screen 2816 clinically used drugs for hCAR activation. Three trials of the experiment in 1536-well plate format were run using 0 μM, 2.5 μM, or 5 μM PK11195 co-treated with varying concentrations of CITCO (A). Luciferase activities from primary screening of the 2816 compounds were normalized and compared with the E_max of CITCO serving as a positive control (B); or categorized based on their EC₅₀ values (C). There were 115 agonists identified and categorized based on their efficacy and potency.