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GSK466317A is a GRK2 inhibitor. GRK2 has been directly implicated in the progression of heart failure. Selective inhibitors of individual subfamilies of G protein-coupled receptor kinases (GRKs) would serve as useful chemical probes as well as leads for therapeutic applications ranging from heart failure to Parkinson's disease.

GSK466317A is a PKA inhibitor, with an IC50 of 12.59 μM. GSK466317A also inhibits GRK1, GRK2, and GRK5, with IC50s of 1000, 31.62, and 39.81 μM, respectively[1].

PKA: 12.59 μM (IC₅₀)

[1] Homan KT, et, al. Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors. ACS Chem Biol. 2015 Jan 16;10(1):310-9. DOI:10.1021/cb5006323