ROCK1
ENSG00000067900
Target class
Kinase
Chromosome
18
Approved drugs
2
Clinical candidates (approved and in development)
11
- Approved drugs
- 2
- Clinical candidates (approved and in development)
- 11
- Chemical probe available
- Yes
- Other names
- p160ROCK
- Target name
- ROCK1
- Gene name
- Rho associated coiled-coil containing protein kinase 1
- Gene symbol
- ROCK1
- Protein name
- Rho-associated protein kinase 1 (EC 2.7.11.39) (Renal carcinoma antigen NY-REN-35) (Rho-associated, coiled-coil-containing protein kinase 1) (Rho-associated, coiled-coil-containing protein kinase I) (ROCK-I) (p160 ROCK-1) (p160ROCK)
- Gene biotype
- Protein coding
- Gene family
- Pleckstrin homology domain containing|Rho associated coiled-coil containing protein kinase family
- Target class
- Kinase
- Target type
- Human gene
- Tissues expressed in
- 54
- Highest tissue expression
- 81.42
- Tissue specificity (Gini)
- 0.419
- Tissue specificity (tau)
- 0.789
- KEGG gene identifiers
- hsa:6093
- Protein interaction confidence
- 0.884415
- Protein interaction partners
- 53
- R-HSA-111465
- R-HSA-3928662
- R-HSA-3928663
- R-HSA-416482
- R-HSA-416572
- R-HSA-4420097
- R-HSA-5627117
- R-HSA-6798695
- R-HSA-8980692
- R-HSA-9013026
- R-HSA-9013106
- R-HSA-9013407
- R-HSA-9013422
- R-HSA-9679191
- R-HSA-9696264
- End position
- 21111813
- Start position
- 20944612
- Chromosome
- 18
- Strand
- Reverse
- Cytoplasm . Cytoplasm, cytoskeleton, microtubule organizing center, centrosome, centriole . Golgi apparatus membrane
- Peripheral membrane protein . Cell projection, bleb . Cytoplasm, cytoskeleton . Cell membrane . Cell projection, lamellipodium . Cell projection, ruffle . Note=A small proportion is associated with Golgi membranes (PubMed:12773565). Associated with the mother centriole and an intercentriolar linker (By similarity). Colocalizes with ITGB1BP1 and ITGB1 at the cell membrane predominantly in lamellipodia and membrane ruffles, but also in retraction fibers (By similarity). Localizes at the cell membrane in an ITGB1BP1-dependent manner (By similarity). .
- PubMed 8617235
- PubMed 12773565
- PubMed 18694941
- Tissue specificity (tau)
- 0.788993
- Expression inequality (Gini)
- 0.419305
Expression in transcripts per million
- Artery - Tibial
- 81.42
- Artery - Coronary
- 49.4
- Artery - Aorta
- 46.23
- Cells - Cultured fibroblasts
- 43.16
- Nerve - Tibial
- 37.59
Expression in transcripts per million
- Artery - Tibial81.42
- Artery - Coronary49.4
- Artery - Aorta46.23
- Cells - Cultured fibroblasts43.16
- Nerve - Tibial37.59
- Cells - EBV-transformed lymphocytes36.69
- Esophagus - Muscularis36.05
- Esophagus - Gastroesophageal Junction35.77
- Adipose - Subcutaneous32.33
- Uterus31.46
- Lung30.25
- Fallopian Tube29.89
- Bladder26.95
- Cervix - Endocervix25.83
- Cervix - Ectocervix24.92
- Breast - Mammary Tissue23.75
- Adipose - Visceral (Omentum)23.39
- Colon - Sigmoid22.78
- Ovary21.91
- Thyroid19.09
- Vagina18.23
- Spleen17.69
- Small Intestine - Terminal Ileum17.52
- Prostate17.18
- Colon - Transverse15.07
And 29 more, listed on the interactive page.
- GO:0006939
- GO:0007159
- GO:0007165
- GO:0007266
- GO:0010508
- GO:0010613
- GO:0010628
- GO:0016525
- GO:0018105
- GO:0022614
- GO:0030036
- GO:0030155
- GO:0030334
- GO:0031175
- GO:0032091
- GO:0032956
- GO:0035556
- GO:0043410
- GO:0045616
- GO:0045664
- GO:0050900
- GO:0050901
- GO:0051045
- GO:0051492
- GO:0051893
And 13 more, listed on the interactive page.
- GO:0000139
- GO:0005576
- GO:0005737
- GO:0005829
- GO:0034774
- GO:0004674
- GO:0005515
- GO:0072518
- GO:0106310
pulmonary hypertension
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- respiratory
PubMed 38773351cardiac arrhythmia
Studies
- cell-based: Listed among thirty kinases critical for cardiomyocyte function based on the following criteria: (1) pharmacological inhibition correlated with cardiomyocyte beat changes, (2) expression in both human-induced pluripotent stemcell-derived cardiomyocytes and adult heart tissue, and (3) effects on cardiomyocyte beating following single gene knockdown.
Biological samples
- cardiovascular system
PubMed 28453775hypotension
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- CV
PubMed 38773351Anxiety
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- CNS
PubMed 38773351GI inflammation
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- GI
PubMed 38773351heart disease
Studies
- preclinical: Important for the heart and vasculature based on findings in genetically modified or kinase-inhibitor-treated mice. Role of kinase in heart/vasculature: Pro-fibrotic and pro-apoptotic in the setting of pressure overload
Biological samples
- cardiovascular system
PubMed 21283106conjunctival hyperaemia
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- ocular
PubMed 38773351hypertrophic cardiomyopathy
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- CV
PubMed 38773351cardiac dysfunction
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- CV
PubMed 38773351lymphatic disorder
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- lymph
PubMed 38773351cytopenia
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- blood/bone marrow
PubMed 38773351anxiety
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- CNS
PubMed 38773351
regulation of catalytic activity
Studies
- biochemical: NVS_ENZ_hROCK1, is one of one assay component(s) measured or calculated from the NVS_ENZ_hROCK1 assay. It is designed to make measurements of enzyme activity, a form of enzyme reporter, as detected with fluorescence intensity signals by Fluorescence and electrophoretic mobility shift technology.
Biological samples
- cell-free
Evidence source
Related records
Trials (115)
- 24-hour Effect of Rocklatan Compared With Latanoprost in Open Angle Glaucoma and Ocular Hypertension Patients
- A 2-Part, Phase 2 Open-label and Crossover Study of Belumosudil for Treatment of Idiopathic Pulmonary Fibrosis
- A Clinical Study to Evaluate the Pharmacokinetics, Efficacy, and Safety of Belumosudil in Chinese Adolescents With cGVHD Who Have Had an Inadequate Response to Glucocorticoids or Other Systemic Therapies
- A Clinical Trial of Safety and Efficacy of Fasudil in Subjects With Amyotrophic Lateral Sclerosis (ALS)
- A Controlled Study of the Aqueous Humor Dynamics of AR-13324 Ophthalmic Solution in Healthy Adult Volunteers
- A Dose Titration Study to Assess the Effects of SAR407899 in Patients With MVA and/or Persistent Stable Angina Despite Angiographically Successful PCI
- A Multi-Center Study on the Use of Rho-Kinase Inhibitor to Reduce or Prevent PVR in RRD Eyes at High Risk for PVR
- A Phase 2 Study Evaluating the Safety and Efficacy of Netarsudil Ophthalmic Solution in Patients With Corneal Edema Due to Fuchs Corneal Dystrophy
- A Phase 2, Double-blind, Placebo-controlled Study of the Efficacy and Safety of Belumosudil in Subjects With Moderate/Severe Chronic Plaque Psoriasis
- A Rho-kinase Inhibitor (Fasudil) in the Treatment of Raynaud's Phenomenon
- A Safety and Tolerability Study of Belumosudil (KD025) Treatment in Subjects With Moderately Severe Psoriasis Vulgaris
- A Single Centre Study to Evaluate 3 Ophthalmic Formulations in Healthy Subjects
- A Study of Belumosudil in Children With Chronic Graft Versus Host Disease (schoolROCK)
- A Study of Belumosudil in People at Risk of Developing Graft-Versus-Host Disease After a Stem Cell Transplant
- A Study of Efficacy and Safety of PHP-201 in Patients With Primary Open Angle Glaucoma or Ocular Hypertension
- A Study to Assess the Effect of Oral Belumosudil on Inhibition of Various Proteins in the Fed State in Healthy Male Subjects
- A Study to Determine the Effect of 500 mg Oral Dose of KD025 in Healthy Male and Post-menopausal Female Subjects
- A Study to Determine the Effect of Multiple Oral Doses and Regimens of KD025 in Healthy Male and Post-menopausal Female Subjects
- A Study to Determine the Effect of Multiple Oral Doses of SLx-2119 in Healthy Male Subjects
- A Study to Evaluate the Safety and Efficacy of K-321 Eye Drops After Descemetorhexis in Participants With Fuchs Endothelial Corneal Dystrophy (FECD)
Drugs (14)
- AMA0076 Rho-associated protein kinase inhibitor
- AT-13148 Rho-associated protein kinase inhibitor
- Belumosudil Rho-associated protein kinase inhibitor
- Belumosudil mesylate Rho-associated protein kinase inhibitor
- DE-104 Rho-associated protein kinase inhibitor
- Fasudil Rho-associated protein kinase inhibitor
- Netarsudil Rho-associated protein kinase inhibitor
- Netarsudil dimesylate Rho-associated protein kinase inhibitor
- Ripasudil Rho-associated protein kinase inhibitor
- Ripasudil hydrochloride dihydrate Rho-associated protein kinase inhibitor
- SAR-407899 Rho-associated protein kinase inhibitor
- SAR-407899 FREE BASE Rho-associated protein kinase inhibitor
- Verosudil Rho-associated protein kinase inhibitor
- Y-39983 Rho-associated protein kinase inhibitor