GRK Assays and Inhibitors

G protein-coupled receptors (GPCRs) are among the most important drug targets in modern medicine. Their activity is tightly regulated by GPCR kinases (GRKs), enzymes that are often overactive in diseases such as cancer and heart failure. Despite strong interest in GRK inhibitors, reliable tools to test their effectiveness directly in living cells have been limited. We have developed a powerful cell-based assay platform that enables precise and isoform-specific analysis of GRK inhibition. Using engineered human cells that express a single GRK alongside a clinically relevant GPCR, our system allows accurate measurement of receptor phosphorylation under physiologically relevant conditions. This makes it possible to directly compare and validate GRK inhibitors in a cellular context. With this approach, we identified highly effective inhibitors for GRK2/3 and GRK5/6, providing validated tools for GPCR research and drug discovery. Our scalable assay platform supports medium- to high-throughput screening and offers a robust solution for companies developing next-generation GRK-targeted therapeutics.