Target family: Rho kinase (type: enzyme)
Target: Rho associated coiled-coil containing protein kinase 2

Ligand: belumosudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2021)
Primary target: yes
Median affinity: 6.980000019073486 pIC50
Reference (Journal): Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin.
Published in: Blood Coagul Fibrinolysis

Ligand: compound 11d [DOI: 10.1039/c0md00194e] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors.
Published in: Medchemcomm

Ligand: compound 22 [PMID: 20462760] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.71999979019165 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: compound 23 [PMID: 35816678] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Identification of a Potent, Selective, and Brain-Penetrant Rho Kinase Inhibitor and its Activity in a Mouse Model of Huntington's Disease.
Published in: J Med Chem

Ligand: compound 32 [PMID: 20471253] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.
Published in: Bioorg Med Chem Lett

Ligand: compound 35 [PMID: 20684608] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.
Published in: J Med Chem

Ligand: compound 8 [PMID: 25898023] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Design, synthesis, and biological evaluation of novel, highly active soft ROCK inhibitors.
Published in: J Med Chem

Ligand: cortistatin A (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.659999847412109 pKd
Reference (Journal): Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11.
Published in: Angew Chem Int Ed Engl

Ligand: fasudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: 1995
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor.
Published in: Hypertension

Ligand: fasudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: 1995
Primary target: yes
Median affinity: 6.570000171661377 pKi
Reference (Journal): Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor.
Published in: Hypertension

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: GSK269962A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.
Published in: J Pharmacol Exp Ther

Ligand: HSD1590 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.949999809265137 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: 9.289999961853027 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: 7.949999809265137 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: 8.699999809265137 pKi
Reference (Journal): Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
Published in: Bioorg Med Chem Lett

Ligand: Rho kinase inhibitor IV (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.929999828338623 pIC50
Reference (Journal): Development of specific Rho-kinase inhibitors and their clinical application.
Published in: Biochim Biophys Acta

Ligand: ripasudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: yes
Median affinity: 7.71999979019165 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: ROCK inhibitor 3 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.109999656677246 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: 6.989999771118164 pIC50
Reference (Journal): Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor.
Published in: Hypertension

Ligand: SAR407899 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.389999866485596 pKi
Reference (Journal): Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor.
Published in: Hypertension

Ligand: SAR407899 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.440000057220459 pKi
Reference (Journal): Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor.
Published in: Hypertension

Ligand: sovesudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.289999961853027 pIC50
Reference (Journal): 3-[2-(Aminomethyl)-5-[(pyridin-4-yl)carbamoyl]phenyl] benzoates as soft ROCK inhibitors.
Published in: Bioorg Med Chem Lett

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:  pKi
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:  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:  pKi
Reference (Journal): Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension.
Published in: Nature

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: zelasudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.519999980926514 pIC50
Reference (Patent): Heterocyclylamino-substituted triazoles as modulators of rho-associated protein kinase