Netarsudil mesylate, the mesylate salt form of Netarsudil (formerly known as AR-13324; Rhopressa), is novel ROCK inhibitor with Ki of 0.2-10.3 nM.

Hydroxyfasudil (also called HA1100 HCl), a metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.

BDP5290 is a novel, potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.

RKI-1313 is a novel and potent inhibitor of the ROCK kinases.

Verosudil (AR-11324; AR 11324; AR11324) is a novel and potent Rho kinase inhibitor with anti-hypertensive activity.

LX7101 (LX-7101; LX 7101) is a novel, potent, pyrrolopyrimidine-based, and topically-usd inhibitor of LIM domain kinase 2 (LIMK2), which is a kinase associated with the regulation of intraocular pressure.

SR-3677 (SR3677) is a potent and selective Rho-kinase/ROCK2 inhibitor with anticancer activity.

Belumosudil mesylate (previously SLx2119; KD025; SLx-2119; KD-025; Rezurock), the mesylate salt of belumosudil, is anorally bioavailable ROCK2 inhibitor approved in 2021 for the treatment of chronic graft versus host disease (cGvHD).

SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nM on isolated human enzyme.

GSK180736A (GSK-180736A) is a GRK2 inhibitor that was developed as a novel and potent Rho-associated, coiled-coil-containing protein kinase (ROCK) inhibitor which binds to GRK2 (G protein-coupled receptor kinase 2) with IC50 of 0.77 μM; G protein-coupled receptors (GPCRs) are central to many physiological processes.