Potent, selective, ATP-competitive, and orally active ROCK inhibitor (in vitro IC50 values 1.69 μM and 0.10 μM for ROCK1 and ROCK2 resp.) that reduces both inflammatory and non-inflammatory pain in rat models. Another group published IC50 values of 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2 respectively. AS 1892802 dose dependently prevented the formation of tibial cartilage lesions due to MIA induction of osteoarthritis (OA), and completely inhibited IL-1α–induced PGE2 production. Additionally, it potently inhibited the phosphorylation of the ROCK substrate MLC2 in intact human breast cancer cells.