Table 2. . Rho kinase inhibitors.
No. | Structure | Inhibitor class | Publication year | Activity |
---|---|---|---|---|
13 | HTS compound | 2008 | IC50 = 7.2 nM | |
14 | Synthetic ‘isoquinoline prototype’ | 1997 | Ki = 330 nM | |
15 | Fasudil derivative approved for glaucoma treatment in Japan | 2014 | ROCK-I (IC50 = 51 nM); ROCK-II (IC50 = 19 nM) | |
16 | Synthetic ‘isoquinoline series’ | 1997 | Ki = 1.6 nM | |
17 | Synthetic ‘4-aminopyridine series’ | 1997 | Ki = 0.14 µM | |
18 | Synthetic ‘pyrrolopyridine series’ | 2007 | ROCK-II (IC50 = 3.6 nM) | |
19 | Synthetic ‘indazole series’ | 2006 | IC50 = 13 nM | |
20 | Synthetic benzadioxane-based compound | 2008 | ROCK-I (IC50 = 56 nM) | |
21 | Tetrahydroisoquinoline-based inhibitor | 2010 | ROCK-II (IC50 <1 nM) | |
22 | Selective ROCK-II inhibitor | 2011 | ROCK-II (IC50 = 1.7 nM) | |
23 | Tricyclic pyridocarboxamide derivatives | 2015 | ROCK-II (IC50 = 1 nM) | |
24 | Structure-based drug design inhibitor | 2014 | IC50 = 1.5 μM | |
25 | Structure-based design inhibitor | 2013 | ROCK-II (IC50 = 0.02 μM) | |
26 | Ligand-based drug design inhibitor | 2011 | ROCK-II (IC50 = 0.02 μM) |
HTS: High-throughput screening; ROCK: Rho kinase.