Experimental IC₅₀ values and transactivation activity of the selected compounds.

<p>A competitive binding assay was used to assess the ability of experimental compounds, FMOC or rosiglitazone to displace a fluorescent PPARγ ligand from a human-derived recombinant PPARγ ligand-binding domain. The concentration of the test compound that results in a half-maximal shift in the polarization value is defined as IC₅₀. This value is a measure of the relative affinity of the test compound for the PPAR ligand-binding domain. The transactivation capacity of selected compounds was also determined in HepG2 cells as described in Materials and Methods. Results represent the mean ± SD of at least three separate experiments performed in triplicate. Results are expressed as arbitrary firefly luciferase units relative to arbitrary renilla luciferase units.</p><p>For compounds C2, C3 and C6, no binding was observed when assayed at concentrations up to 8 mM. Compounds C4 and C10 were not assayed because of solubility problems. For Rosiglitazone and FMOC, gene reporter activity at 500 and 1000 μM were not assayed because of solubility problems.</p>**<p>p<0.001 and * p<0.05 when compared to the control (DMSO) in an ANOVA test.