Endogenous Receptor Evaluations: Gi- and Gs-Coupled GPCR Receptor Subtyping and Schild Analysis

G-protein coupled receptors (GPCRs) remain among the most important drug targets in the biopharmaceutical industry, and are proving to be highly complex in their signaling behaviors. Capturing this complexity in the early stages of drug discovery is critical and is best done by investigating endogenously expressed targets in live cells. In this application note the ability of the CellKey® System, a label-free cell based assay platform from Molecular Devices, to reliably and robustly measure endogenous receptors, including complex Gi- and Gs-coupled receptors, is demonstrated. The high sensitivity of the CellKey System allows flexibility in choosing cell lines and primary cells which express Gi- and Gs-GPCRs of interest, thus providing access to more biologically relevant contexts for experimental analyses.