CCG-22440 is a Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitor. CCG-224406 had an IC50 for GRK2 of 130 nM, greater than 700-fold selectivity over other GRK subfamilies, and no detectable inhibition of ROCK1. G protein-coupled receptors (GPCRs) are central to many physiological processes. Regulation of this superfamily of receptors is controlled by GPCR kinases (GRKs), some of which have been implicated in heart failure.
