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. 2017 Aug 8;3(4):FSO204. doi: 10.4155/fsoa-2017-0010

Table 2. . Rho kinase inhibitors.

No. Structure Inhibitor class Publication year Activity
13 graphic file with name fsoa-03-204-T2a.gif HTS compound 2008 IC50 = 7.2 nM

14 graphic file with name fsoa-03-204-T2b.gif Synthetic ‘isoquinoline prototype’ 1997 Ki = 330 nM

15 graphic file with name fsoa-03-204-T2c.gif Fasudil derivative approved for glaucoma treatment in Japan 2014 ROCK-I (IC50 = 51 nM); ROCK-II (IC50 = 19 nM)

16 graphic file with name fsoa-03-204-T2d.gif Synthetic ‘isoquinoline series’ 1997 Ki = 1.6 nM

17 graphic file with name fsoa-03-204-T2e.gif Synthetic ‘4-aminopyridine series’ 1997 Ki = 0.14 µM

18 graphic file with name fsoa-03-204-T2f.gif Synthetic ‘pyrrolopyridine series’ 2007 ROCK-II (IC50 = 3.6 nM)

19 graphic file with name fsoa-03-204-T2g.gif Synthetic ‘indazole series’ 2006 IC50 = 13 nM

20 graphic file with name fsoa-03-204-T2h.gif Synthetic benzadioxane-based compound 2008 ROCK-I (IC50 = 56 nM)

21 graphic file with name fsoa-03-204-T2i.gif Tetrahydroisoquinoline-based inhibitor 2010 ROCK-II (IC50 <1 nM)

22 graphic file with name fsoa-03-204-T2j.gif Selective ROCK-II inhibitor 2011 ROCK-II (IC50 = 1.7 nM)

23 graphic file with name fsoa-03-204-T2k.gif Tricyclic pyridocarboxamide derivatives 2015 ROCK-II (IC50 = 1 nM)

24 graphic file with name fsoa-03-204-T2l.gif Structure-based drug design inhibitor 2014 IC50 = 1.5 μM

25 graphic file with name fsoa-03-204-T2m.gif Structure-based design inhibitor 2013 ROCK-II (IC50 = 0.02 μM)

26 graphic file with name fsoa-03-204-T2n.gif Ligand-based drug design inhibitor 2011 ROCK-II (IC50 = 0.02 μM)

HTS: High-throughput screening; ROCK: Rho kinase.