abstract |
The present invention provides a method of high-throughput screening (HTS) of active agents of a cell-surface G-Protein coupled receptor (GPCR) or another target receptor of interest. The method uses a non-invasive, sensitive reporting system that is proximal to the target of interest, combined with a dynamic, automated screening procedure so as to detect orthosteric ligands, such as agonists and antagonists, but is also suitable to detect allosteric or low affinity active agents of a GPCR and possibly other disease-related receptors. |