Binding assays for identifying ligands that modulate human T1R3 polypeptide-associated taste are disclosed. These assays detect the specific binding of compounds to a human T1R3 polypeptide or the modulation of the specific binding of another compound that specifically binds human T1R3 polypeptide. The binding assays may include the use of detectable labels, e.g., radionuclides, enzymes, fluorophores, and the like. Compounds identified in these binding assays have potential application as T1R3 taste modulators and therefore potentially are useful additives in compositions for human or animal consumption.