G protein-coupled receptor kinases (GRKs, GPCRKs) are a family of protein kinases within the AGC (protein kinase A, protein kinase G, protein kinase C) group of kinases. Like all AGC kinases, GRKs use ATP to add phosphate to serine and threonine residues in specific locations of target proteins. In particular, GRKs phosphorylate intracellular domains of G protein-coupled receptors (GPCRs). GRKs function in tandem with arrestin proteins to regulate the sensitivity of GPCRs for stimulating downstream heterotrimeric G protein and G protein-independent signaling pathways.
|CSN22551||GSK180736A||817194-38-0||GSK180736A is an inhibitor of G protein-coupled receptor kinase 2 (GRK2) with IC50 of 0.77 μM.|
|CSN19161||CCG-215022||1813527-81-9||CCG-215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, 5 and 1, respectively.|