A recombinant Huh7-PPRE-Luc cell line, carrying a peroxisome proliferator response element (PPRE)-driven luciferase gene, is an efficient tool for evaluation of potential peroxisome proliferator-activated receptor (PPAR) agonists. The cells exhibited a good dose–response induction in PPRE-driven luciferase activity by three subtypes of PPAR agonists as well as by a retinoid X receptor agonist, 9-cis-retinoic acid. Here, the bioassay is fitted into a 96-well plate format for high-throughput screening purpose.