The assay discusses the potential for small molecule modulators of the "regulator of G-protein signaling" (RGS) protein superfamily to enhance GPCR signaling pathways and increase the specificity of therapeutics. RGS proteins deactivate G-protein alpha subunits, and inhibitors of the RGS domain could be combined with GPCR agonists to potentiate cellular responses. These modulators could be useful in treating CNS disorders through the regulation of the diverse and dynamic distribution of RGS proteins in the human brain. Is the molecule effective to this assay?