A method for screening G-protein coupled receptor ligands is provided, thereby improving speed and accuracy of the screening by using fluorescence polarization assay. The method for screening G-protein coupled receptor ligands comprises the steps of: (a) diluting the G-protein coupled receptors(GPCRs) with a buffer solution containing surfactant; (b) mixing a testing material, a fluorescence-labeled neuropeptide tracer and G-protein coupled receptors(GPCRs), sequentially, and reacting them; and (c) measuring fluorescence polarization of the reaction product of step (b) at 0.5 to 24 hours, wherein the G-protein coupled receptor is neuropeptide FF(NPFF) receptor; and the surfactant is Pluronic F-127 or Tween 20.
Method for screening of G-protein coupled receptor ligands