Assays for Allosteric Modulators of G-Protein Coupled Receptors (GPCRs)

摘要

The present invention relates to G protein-coupled receptors (GPCRs) and allosteric modulators thereof. More specifically, the invention relates to allosteric modulators of GPCRs that interact at an intracellular binding site. It also relates to methods for designing or identifying small molecule allosteric modulators, including assays (such as competitive binding assays) and methods employing a homology model for the GPCR intracellular site.