The PPARγ Ligand Screening Assay Kit provides a single step fluorescence-based assay for screening potential PPARγ-specific ligands. The assay utilizes the ability of potential PPARγ-binding ligands to displace a fluorescent probe, which has a strong affinity for PPARγ Ligand Binding Domain, resulting in loss of fluorescence of the probe. The relative drop in the fluorescence, as a result of competitive binding of PPARγ ligand, can be correlated to the affinity (and hence IC50) of the PPARγ candidate ligand. The PPARγ Ligand Screening Assay Kit is easy to use, faster and more convenient as compared to Fluorescence Polarization and TR-FRET-based screening methods. The assay kit can be used to identify and characterize PPARγ-specific ligands for therapeutic applications.