Target family: Rho kinase (type: enzyme)
Target: Rho associated coiled-coil containing protein kinase 1

Ligand: fasudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: 1995
Primary target: yes
Median affinity: 7 pKi
Reference (Journal): Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: GSK269962A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.800000190734863 pIC50
Reference (Journal): Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.
Published in: J Pharmacol Exp Ther

Ligand: GSK429286A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.849999904632568 pIC50
Reference (Journal): Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors.
Published in: J Med Chem

Ligand: HSD1590 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.779999732971191 pKd
Reference (Journal): Potently inhibiting cancer cell migration with novel 3H-pyrazolo[4,3-f]quinoline boronic acid ROCK inhibitors.
Published in: Eur J Med Chem

Ligand: HSD1590 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.90999984741211 pIC50
Reference (Journal): Potently inhibiting cancer cell migration with novel 3H-pyrazolo[4,3-f]quinoline boronic acid ROCK inhibitors.
Published in: Eur J Med Chem

Ligand: netarsudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2019)
Primary target: no
Median affinity: 7.489999771118164 pIC50
Reference (Journal): Potently inhibiting cancer cell migration with novel 3H-pyrazolo[4,3-f]quinoline boronic acid ROCK inhibitors.
Published in: Eur J Med Chem

Ligand: ripasudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: yes
Median affinity: 7.289999961853027 pIC50
Reference (Journal): Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits.
Published in: Curr Eye Res

Ligand: RKI-1447 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
Published in: Medchemcomm

Ligand: fasudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: 1995
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: Y27632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.
Published in: Bioorg Med Chem Lett

Ligand: ROCK inhibitor 3 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): Pharmacological characterization of a highly selective Rho kinase (ROCK) inhibitor and its therapeutic effects in experimental pulmonary hypertension.
Published in: Eur J Pharmacol

Ligand: SAR407899 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.559999942779541 pIC50
Reference (Journal): Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor.
Published in: Hypertension

Ligand: verosudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Ocular hypotensive effect of the Rho kinase inhibitor AR-12286 in patients with glaucoma and ocular hypertension.
Published in: Am J Ophthalmol

Ligand: Y27632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor.
Published in: Hypertension

Ligand: Y27632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.849999904632568 pKi
Reference (Journal): Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension.
Published in: Nature