Methods for identifying compounds that regulate beta-arrestin signaling complexes

A method of screening a candidate compound for βArrestin mediated anti-G protein coupled receptor signaling activity is comprises: (a) contacting said candidate compound to a βArrestin signaling complex or a constituent thereof, under conditions in which a signaling complex is formed; and then (b) detecting the presence or absence of disruption of said signaling complex, disruption of said complex indicating said compound has βArrestin mediated anti-G protein coupled receptor signaling activity. Compositions and kits for carrying out the method are also described.