Table 1.

Current Investigational Rho Kinase Inhibitors

Agent and Reference	Chemical Formula and Structure	ROCK1 IC50 (nM)	ROCK2 IC50 (nM)	Effect on Other Receptors	Year Introduced	Current Phase
HA-107725–28 C14H17N3O2S		NA	NA	PKA, PKG, PKC	1995	Phase 1
Y-276322 C14H12N3O.2HCL		42	71	PKA, PKC, MLCK	1997	Preclinical
H-1152P33–35 C16H21N3O2S		NA	12	PKC, AMPK	1999	Preclinical
INS-11564436,37 C20H29NO5S		5	14	NA	2004	Phase 1
Y-3998338–40 C16H17C1N4O		3.6	3.6	NA	2005	Phase 2
SB772077BS41,42 C15H18N8O2		5.6	5.6	NA	2007	Preclinical
LX710143–46 C23H29N7O3		69	32	LIMK, Akt1	2007	Phase 1/Phase 2
AR-1228647–52 C17H17N3O2S		NA	NA	NA	2009	Phase 2
AMA-007644–54	NA	3.7	2.3	NA	2011	Phase 2
RKI 144755,56 C16H14N4O2S		14.5	6.2	NA	2012	Preclinical
AR-1353357	NA	NA	NA	NET	2013	Preclinical
AMA052658,59	NA	5.7	3.1	NA	2013	Preclinical
H-133760–62		NA	NA	PKA, PKN2, PKD1, LRRK2	2015	Phase 2
ITRI-E-21263	NA	NA	3.2	NA	2017	Preclinical
ITRI-E-24764	Unavailable	NA	10.9	NA	2017	Preclinical

Note: IC₅₀ is the half-maximal inhibitory concentration (the amount of drug needed to inhibit, in vitro, a given biological process or biological component by 50%).

Abbreviations: nM, nanomolar; NA, not available; PKA, protein kinase A; PKC, protein kinase C; MLCK, myosin light chain kinase; NET, norepinephrine transporter; LIMK, LIM kinase; GRK, G-protein coupled receptor kinase; LRRK, Leucine-rich repeat kinase 2; AMPK, 5ʹ adenosine monophosphate-activated protein kinase.