GRK

CCG215022 is a potent GRK2 and GRK5 inhibitor. CCG215022 exhibited nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA.

CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively).

GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.

GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.

Takeda103A is a potent GRK2-dependent bovine tubulin oxidation inhibitor.