Drug intelligence / Profile preview

Vertex ROCK inhibitor compound 22

Development stage
Preclinical
Lead developer
Vertex
Modality
Small Molecules
Administration
Ophthalmic, Oral
01

Overview

Vertex ROCK inhibitor compound 22 is a potent, small molecule inhibitor of Rho-associated coiled-coil-containing protein kinases 1 and 2 (ROCK1 and ROCK2), originally identified by Vertex Pharmaceuticals during structure-activity relationship (SAR) studies. The compound functions by binding to the ATP-binding pocket of the ROCK catalytic domain, thereby preventing the phosphorylation of downstream substrates involved in cytoskeletal regulation. By inhibiting ROCK signaling, the molecule influences critical cellular functions such as actin filament organization, cell migration, and smooth muscle contraction. Due to these effects, it has been investigated for therapeutic potential in treating glaucoma (by enhancing aqueous humor outflow), cardiovascular diseases (through vasodilation and reduction of vascular resistance), and cancer (by hindering tumor cell invasion and metastasis).

Other names
Vertex compound 22
02

Targets

ROCK1 (Rho-associated coiled-coil containing protein kinase 1)

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