Compounds > ar-12286
Page last updated: 2024-11-13

ar-12286

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Description

AR-12286: a Rho kinase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID66906051
CHEMBL ID3545065
SCHEMBL ID1097105
SCHEMBL ID19235657
MeSH IDM0585608

Synonyms (34)

Synonym
SCHEMBL1097105
1414854-42-4
ar-12286
verosudil [usan:inn]
(2rs)-2-(dimethylamino)-n-(1-oxo-1,2-dihydroisoquinolin-6-yl)-2-(thiophen-3-yl)acetamide
ar 12286
unii-maf34143wm
verosudil
maf34143wm ,
D10737
verosudil (usan/inn)
verosudil [inn]
ar-12286 free base
verosudil [usan]
3-thiopheneacetamide, n-(1,2-dihydro-1-oxo-6-isoquinolinyl)-.alpha.-(dimethylamino)-
verosudil [who-dd]
CHEMBL3545065
2-(dimethylamino)-n-(1-oxo-2h-isoquinolin-6-yl)-2-thiophen-3-ylacetamide
gtpl8911
verosudil(ar-12286)
SCHEMBL19235657
AKOS032960471
1414854-42-4 (free base)
2-(dimethylamino)-n-(1-oxo- 1,2-dihydroisoquinolin-6-yl)-2-(thiophen-3-yl)acetamide
Q27089140
SB17090
CS-0012352
AMY42175
MS-24894
HY-16758
A857572
n-(1,2-dihydro-1-oxo-6-isoquinolinyl)-alpha-(dimethylamino)-3-thiopheneacetamide
DTXSID801336680
bdbm50601415

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The most frequent ocular adverse events were conjunctival hyperaemia, eye irritation, instillation site reaction, increased lacrimation, and blurred vision which were relatively short-lived and judged as not clinically significant."( Ocular hypotensive efficacy, safety and systemic absorption of AR-12286 ophthalmic solution in normal volunteers.
Kopczynski, C; Novack, GD; Swearingen, D; van Haarlem, T, 2013)		0.63

Bioavailability

ExcerptReferenceRelevance
" Ester 60 improved bioavailability of its parent ROCK inhibitor, 29 (Ki=0."( Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
deLong, MA; Heintzelman, GR; Kopczynski, CC; Laethem, CL; Lin, CW; Moore, LA; Royalty, SM; Sherman, B; Sturdivant, JM; Yingling, JD, 2016)		0.43

Dosage Studied

ExcerptRelevanceReference
" Dosing was once-daily in the morning for 7 days, then once-daily in the evening for 7 days, then twice daily for 7 days."( Ocular hypotensive effect of the Rho kinase inhibitor AR-12286 in patients with glaucoma and ocular hypertension.
Kopczynski, C; Novack, GD; van Haarlem, T; Williams, RD, 2011)		0.62
"25% AR-12286 after twice daily dosing (up to -6."( Ocular hypotensive effect of the Rho kinase inhibitor AR-12286 in patients with glaucoma and ocular hypertension.
Kopczynski, C; Novack, GD; van Haarlem, T; Williams, RD, 2011)		1.18
" Volunteers were randomised to one of two dosing sequences: Formulation A once daily, both eyes (OU) for 8 days, a 7-day minimum washout, and then Formulation B, or the reverse."( Ocular hypotensive efficacy, safety and systemic absorption of AR-12286 ophthalmic solution in normal volunteers.
Kopczynski, C; Novack, GD; Swearingen, D; van Haarlem, T, 2013)		0.63
"5%, dosed once daily in the morning for 8 days."( Ocular hypotensive efficacy, safety and systemic absorption of AR-12286 ophthalmic solution in normal volunteers.
Kopczynski, C; Novack, GD; Swearingen, D; van Haarlem, T, 2013)		0.63
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Rho-associated protein kinase 2Homo sapiens (human)Ki0.00200.00200.23310.3300AID1894031
Rho-associated protein kinase 1Homo sapiens (human)Ki0.00200.00200.30672.2000AID1894030
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (86)

Processvia Protein(s)Taxonomy
epithelial to mesenchymal transitionRho-associated protein kinase 2Homo sapiens (human)
positive regulation of protein phosphorylationRho-associated protein kinase 2Homo sapiens (human)
response to ischemiaRho-associated protein kinase 2Homo sapiens (human)
aortic valve morphogenesisRho-associated protein kinase 2Homo sapiens (human)
protein phosphorylationRho-associated protein kinase 2Homo sapiens (human)
smooth muscle contractionRho-associated protein kinase 2Homo sapiens (human)
canonical NF-kappaB signal transductionRho-associated protein kinase 2Homo sapiens (human)
positive regulation of endothelial cell migrationRho-associated protein kinase 2Homo sapiens (human)
positive regulation of cardiac muscle hypertrophyRho-associated protein kinase 2Homo sapiens (human)
positive regulation of gene expressionRho-associated protein kinase 2Homo sapiens (human)
negative regulation of gene expressionRho-associated protein kinase 2Homo sapiens (human)
positive regulation of centrosome duplicationRho-associated protein kinase 2Homo sapiens (human)
negative regulation of angiogenesisRho-associated protein kinase 2Homo sapiens (human)
actin cytoskeleton organizationRho-associated protein kinase 2Homo sapiens (human)
regulation of cell adhesionRho-associated protein kinase 2Homo sapiens (human)
positive regulation of cell migrationRho-associated protein kinase 2Homo sapiens (human)
cortical actin cytoskeleton organizationRho-associated protein kinase 2Homo sapiens (human)
regulation of nervous system processRho-associated protein kinase 2Homo sapiens (human)
positive regulation of connective tissue growth factor productionRho-associated protein kinase 2Homo sapiens (human)
regulation of actin cytoskeleton organizationRho-associated protein kinase 2Homo sapiens (human)
negative regulation of myosin-light-chain-phosphatase activityRho-associated protein kinase 2Homo sapiens (human)
regulation of circadian rhythmRho-associated protein kinase 2Homo sapiens (human)
positive regulation of MAPK cascadeRho-associated protein kinase 2Homo sapiens (human)
modulation by host of viral processRho-associated protein kinase 2Homo sapiens (human)
negative regulation of nitric oxide biosynthetic processRho-associated protein kinase 2Homo sapiens (human)
regulation of keratinocyte differentiationRho-associated protein kinase 2Homo sapiens (human)
rhythmic processRho-associated protein kinase 2Homo sapiens (human)
centrosome duplicationRho-associated protein kinase 2Homo sapiens (human)
regulation of stress fiber assemblyRho-associated protein kinase 2Homo sapiens (human)
positive regulation of stress fiber assemblyRho-associated protein kinase 2Homo sapiens (human)
regulation of focal adhesion assemblyRho-associated protein kinase 2Homo sapiens (human)
mRNA destabilizationRho-associated protein kinase 2Homo sapiens (human)
negative regulation of biomineral tissue developmentRho-associated protein kinase 2Homo sapiens (human)
cellular response to testosterone stimulusRho-associated protein kinase 2Homo sapiens (human)
response to transforming growth factor betaRho-associated protein kinase 2Homo sapiens (human)
protein localization to plasma membraneRho-associated protein kinase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionRho-associated protein kinase 2Homo sapiens (human)
blood vessel diameter maintenanceRho-associated protein kinase 2Homo sapiens (human)
regulation of angiotensin-activated signaling pathwayRho-associated protein kinase 2Homo sapiens (human)
negative regulation of protein localization to lysosomeRho-associated protein kinase 2Homo sapiens (human)
regulation of cellular response to hypoxiaRho-associated protein kinase 2Homo sapiens (human)
positive regulation of amyloid-beta formationRho-associated protein kinase 2Homo sapiens (human)
positive regulation of protein localization to early endosomeRho-associated protein kinase 2Homo sapiens (human)
positive regulation of amyloid precursor protein catabolic processRho-associated protein kinase 2Homo sapiens (human)
regulation of establishment of endothelial barrierRho-associated protein kinase 2Homo sapiens (human)
negative regulation of bicellular tight junction assemblyRho-associated protein kinase 2Homo sapiens (human)
cellular response to acetylcholineRho-associated protein kinase 2Homo sapiens (human)
positive regulation of connective tissue replacementRho-associated protein kinase 2Homo sapiens (human)
response to angiotensinRho-associated protein kinase 2Homo sapiens (human)
regulation of establishment of cell polarityRho-associated protein kinase 2Homo sapiens (human)
regulation of cell motilityRho-associated protein kinase 2Homo sapiens (human)
actomyosin structure organizationRho-associated protein kinase 2Homo sapiens (human)
peptidyl-threonine phosphorylationRho-associated protein kinase 2Homo sapiens (human)
mitotic cytokinesisRho-associated protein kinase 2Homo sapiens (human)
embryonic morphogenesisRho-associated protein kinase 2Homo sapiens (human)
regulation of cell junction assemblyRho-associated protein kinase 2Homo sapiens (human)
Rho protein signal transductionRho-associated protein kinase 2Homo sapiens (human)
epithelial to mesenchymal transitionRho-associated protein kinase 1Homo sapiens (human)
aortic valve morphogenesisRho-associated protein kinase 1Homo sapiens (human)
apical constrictionRho-associated protein kinase 1Homo sapiens (human)
protein phosphorylationRho-associated protein kinase 1Homo sapiens (human)
smooth muscle contractionRho-associated protein kinase 1Homo sapiens (human)
leukocyte cell-cell adhesionRho-associated protein kinase 1Homo sapiens (human)
signal transductionRho-associated protein kinase 1Homo sapiens (human)
canonical NF-kappaB signal transductionRho-associated protein kinase 1Homo sapiens (human)
Rho protein signal transductionRho-associated protein kinase 1Homo sapiens (human)
positive regulation of autophagyRho-associated protein kinase 1Homo sapiens (human)
positive regulation of cardiac muscle hypertrophyRho-associated protein kinase 1Homo sapiens (human)
positive regulation of gene expressionRho-associated protein kinase 1Homo sapiens (human)
positive regulation of phosphatase activityRho-associated protein kinase 1Homo sapiens (human)
negative regulation of angiogenesisRho-associated protein kinase 1Homo sapiens (human)
peptidyl-serine phosphorylationRho-associated protein kinase 1Homo sapiens (human)
membrane to membrane dockingRho-associated protein kinase 1Homo sapiens (human)
actin cytoskeleton organizationRho-associated protein kinase 1Homo sapiens (human)
regulation of cell adhesionRho-associated protein kinase 1Homo sapiens (human)
regulation of cell migrationRho-associated protein kinase 1Homo sapiens (human)
cortical actin cytoskeleton organizationRho-associated protein kinase 1Homo sapiens (human)
neuron projection developmentRho-associated protein kinase 1Homo sapiens (human)
bleb assemblyRho-associated protein kinase 1Homo sapiens (human)
negative regulation of protein bindingRho-associated protein kinase 1Homo sapiens (human)
regulation of actin cytoskeleton organizationRho-associated protein kinase 1Homo sapiens (human)
positive regulation of dephosphorylationRho-associated protein kinase 1Homo sapiens (human)
negative regulation of myosin-light-chain-phosphatase activityRho-associated protein kinase 1Homo sapiens (human)
negative regulation of phosphorylationRho-associated protein kinase 1Homo sapiens (human)
positive regulation of MAPK cascadeRho-associated protein kinase 1Homo sapiens (human)
regulation of keratinocyte differentiationRho-associated protein kinase 1Homo sapiens (human)
regulation of neuron differentiationRho-associated protein kinase 1Homo sapiens (human)
leukocyte migrationRho-associated protein kinase 1Homo sapiens (human)
leukocyte tethering or rollingRho-associated protein kinase 1Homo sapiens (human)
negative regulation of membrane protein ectodomain proteolysisRho-associated protein kinase 1Homo sapiens (human)
myoblast migrationRho-associated protein kinase 1Homo sapiens (human)
regulation of stress fiber assemblyRho-associated protein kinase 1Homo sapiens (human)
regulation of focal adhesion assemblyRho-associated protein kinase 1Homo sapiens (human)
positive regulation of focal adhesion assemblyRho-associated protein kinase 1Homo sapiens (human)
mRNA destabilizationRho-associated protein kinase 1Homo sapiens (human)
negative regulation of biomineral tissue developmentRho-associated protein kinase 1Homo sapiens (human)
regulation of microtubule cytoskeleton organizationRho-associated protein kinase 1Homo sapiens (human)
response to transforming growth factor betaRho-associated protein kinase 1Homo sapiens (human)
protein localization to plasma membraneRho-associated protein kinase 1Homo sapiens (human)
regulation of synapse maturationRho-associated protein kinase 1Homo sapiens (human)
podocyte cell migrationRho-associated protein kinase 1Homo sapiens (human)
motor neuron apoptotic processRho-associated protein kinase 1Homo sapiens (human)
blood vessel diameter maintenanceRho-associated protein kinase 1Homo sapiens (human)
regulation of angiotensin-activated signaling pathwayRho-associated protein kinase 1Homo sapiens (human)
neuron projection arborizationRho-associated protein kinase 1Homo sapiens (human)
positive regulation of amyloid-beta clearanceRho-associated protein kinase 1Homo sapiens (human)
regulation of synaptic vesicle endocytosisRho-associated protein kinase 1Homo sapiens (human)
negative regulation of amyloid-beta formationRho-associated protein kinase 1Homo sapiens (human)
negative regulation of amyloid precursor protein catabolic processRho-associated protein kinase 1Homo sapiens (human)
regulation of establishment of endothelial barrierRho-associated protein kinase 1Homo sapiens (human)
negative regulation of bicellular tight junction assemblyRho-associated protein kinase 1Homo sapiens (human)
positive regulation of connective tissue replacementRho-associated protein kinase 1Homo sapiens (human)
response to angiotensinRho-associated protein kinase 1Homo sapiens (human)
regulation of establishment of cell polarityRho-associated protein kinase 1Homo sapiens (human)
regulation of cell motilityRho-associated protein kinase 1Homo sapiens (human)
negative regulation of motor neuron apoptotic processRho-associated protein kinase 1Homo sapiens (human)
regulation of cell junction assemblyRho-associated protein kinase 1Homo sapiens (human)
mitotic cytokinesisRho-associated protein kinase 1Homo sapiens (human)
embryonic morphogenesisRho-associated protein kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylationRho-associated protein kinase 1Homo sapiens (human)
actomyosin structure organizationRho-associated protein kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
protease bindingRho-associated protein kinase 2Homo sapiens (human)
RNA bindingRho-associated protein kinase 2Homo sapiens (human)
protein serine/threonine kinase activityRho-associated protein kinase 2Homo sapiens (human)
structural molecule activityRho-associated protein kinase 2Homo sapiens (human)
protein bindingRho-associated protein kinase 2Homo sapiens (human)
ATP bindingRho-associated protein kinase 2Homo sapiens (human)
small GTPase bindingRho-associated protein kinase 2Homo sapiens (human)
metal ion bindingRho-associated protein kinase 2Homo sapiens (human)
tau protein bindingRho-associated protein kinase 2Homo sapiens (human)
tau-protein kinase activityRho-associated protein kinase 2Homo sapiens (human)
endopeptidase activator activityRho-associated protein kinase 2Homo sapiens (human)
Rho-dependent protein serine/threonine kinase activityRho-associated protein kinase 2Homo sapiens (human)
protein serine kinase activityRho-associated protein kinase 2Homo sapiens (human)
protein kinase activityRho-associated protein kinase 1Homo sapiens (human)
protein serine/threonine kinase activityRho-associated protein kinase 1Homo sapiens (human)
protein bindingRho-associated protein kinase 1Homo sapiens (human)
ATP bindingRho-associated protein kinase 1Homo sapiens (human)
small GTPase bindingRho-associated protein kinase 1Homo sapiens (human)
metal ion bindingRho-associated protein kinase 1Homo sapiens (human)
tau protein bindingRho-associated protein kinase 1Homo sapiens (human)
tau-protein kinase activityRho-associated protein kinase 1Homo sapiens (human)
Rho-dependent protein serine/threonine kinase activityRho-associated protein kinase 1Homo sapiens (human)
protein serine kinase activityRho-associated protein kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
nucleusRho-associated protein kinase 2Homo sapiens (human)
centrosomeRho-associated protein kinase 2Homo sapiens (human)
cytosolRho-associated protein kinase 2Homo sapiens (human)
plasma membraneRho-associated protein kinase 2Homo sapiens (human)
cytoplasmic ribonucleoprotein granuleRho-associated protein kinase 2Homo sapiens (human)
centrosomeRho-associated protein kinase 2Homo sapiens (human)
cytoskeletonRho-associated protein kinase 2Homo sapiens (human)
cytoplasmRho-associated protein kinase 2Homo sapiens (human)
Golgi membraneRho-associated protein kinase 1Homo sapiens (human)
ruffleRho-associated protein kinase 1Homo sapiens (human)
extracellular regionRho-associated protein kinase 1Homo sapiens (human)
centrioleRho-associated protein kinase 1Homo sapiens (human)
cytosolRho-associated protein kinase 1Homo sapiens (human)
cytoskeletonRho-associated protein kinase 1Homo sapiens (human)
plasma membraneRho-associated protein kinase 1Homo sapiens (human)
cytoplasmic stress granuleRho-associated protein kinase 1Homo sapiens (human)
lamellipodiumRho-associated protein kinase 1Homo sapiens (human)
blebRho-associated protein kinase 1Homo sapiens (human)
secretory granule lumenRho-associated protein kinase 1Homo sapiens (human)
Schaffer collateral - CA1 synapseRho-associated protein kinase 1Homo sapiens (human)
cytoskeletonRho-associated protein kinase 1Homo sapiens (human)
cytoplasmRho-associated protein kinase 1Homo sapiens (human)
cytoplasmic stress granuleRho-associated protein kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID1295082Inhibition of human CYP3A4 at 10 uM2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
AID1894030Inhibition of ROCK1 (unknown origin)2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
AID1295080Inhibition of human CYP2C19 at 10 uM2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
AID1295078Inhibition of human norepinephrine transporter at 10 uM2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
AID1894031Inhibition of ROCK2 (unknown origin)2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
AID1295081Inhibition of human CYP2D6 at 10 uM2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
AID1295079Inhibition of human SERT at 10 uM2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
AID1295068Antiglaucoma activity in Dutch Belted rabbit assessed as decrease in intraocular pressure drug administered 0.1% on day 1 followed 0.3% on day 2 via topical occular instillation measured 8 hrs post dose on day 2 by pneumatonometer2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
AID1295067Antiglaucoma activity in Dutch Belted rabbit assessed as decrease in intraocular pressure drug administered 0.1% on day 1 followed 0.3% on day 2 via topical occular instillation measured 2 hrs post dose on day 2 by pneumatonometer2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
AID1345327Human Rho associated coiled-coil containing protein kinase 2 (Rho kinase)2011American journal of ophthalmology, Nov, Volume: 152, Issue:5
Ocular hypotensive effect of the Rho kinase inhibitor AR-12286 in patients with glaucoma and ocular hypertension.
AID1345316Human Rho associated coiled-coil containing protein kinase 1 (Rho kinase)2011American journal of ophthalmology, Nov, Volume: 152, Issue:5
Ocular hypotensive effect of the Rho kinase inhibitor AR-12286 in patients with glaucoma and ocular hypertension.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (66.67)24.3611
2020's2 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.54

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.54 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.54)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (50.00%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other2 (33.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		3.4110aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
paroxetine
Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.		3.4110aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
y 27632
Y 27632: RN given for di-HCl salt; inhibits Rho-associated protein kinase; inhibits calcium sensitization to affect smooth muscle relaxation; structure in first source. Y-27632 : A monocarboxylic acid amide that is trans-[(1R)-1-aminoethyl]cyclohexanecarboxamide in which one of the nitrogens of the aminocarbony group is substituted by a pyridine nucleus. It has been shown to exhibit inhibitory activity against Rho-associated protein kinase (ROCK) enzyme.		3.4110aromatic amide
bosutinib
4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile: a Src kinase inhibitor; structure in first source		3.4110aminoquinoline;
aromatic ether;
dichlorobenzene;
N-methylpiperazine;
nitrile;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
y-39983
Y-39983: SNJ-1656 is an ophthalmic solution of Y-39983; ROCK (rho kinase) inhibitor, promotes regeneration of crushed axons of retinal ganglion cells; structure in first source		3.4110pyrrolopyridine
ripasudil
[no description available]		3.4110isoquinolines
tofacitinib
tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.		3.4110N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
masitinib
[no description available]		3.41101,3-thiazoles;
benzamides;
N-alkylpiperazine;
pyridines		antineoplastic agent;
antirheumatic drug;
tyrosine kinase inhibitor
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
[no description available]		3.4110methoxybenzenes;
substituted aniline
np 031112
tideglusib: an NSAID and neuroprotective agent. tideglusib : A member of the class of thiadiazolidines that is 1,2,4-thiadiazolidine-3,5-dione which is substituted by a naphthalen-1-yl group at position 2 and by a benzyl group at position 4. It is a non-ATP competitive inhibitor of glycogen synthase kinase 3beta (GSK3beta) and has neuroprotective effects. Currently under clinical investigation for the treatment of Alzheimer's disease and progressive supranuclear palsy.		3.4110benzenes;
naphthalenes;
thiadiazolidine		anti-inflammatory agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent
pf 573228
6-(4-(3-(methylsulfonyl)benzylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one: structure in first source		3.4110quinolines
pha 767491
PHA 767491: a Cdc7 inhibitor; structure in first source		3.4110pyrrolopyridine
fedratinib
fedratinib: a selective small-molecule inhibitor of JAK2		3.4110sulfonamide
N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonyl-1-piperazinyl)-1-piperidinyl]anilino]-4-pyrimidinyl]-2-imidazo[1,2-a]pyridinyl]-2-methoxybenzamide
[no description available]		3.4110benzamides
baricitinib
[no description available]		3.4110azetidines;
nitrile;
pyrazoles;
pyrrolopyrimidine;
sulfonamide		anti-inflammatory agent;
antirheumatic drug;
antiviral agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
immunosuppressive agent
pf 3644022
[no description available]		3.4110
gsk2292767
GSK2292767: inhibits phosphoinositide 3-kinase delta; structure in first source		3.4110
bay 65-1942
[no description available]		3.4110
ConditionIndicatedRelationship StrengthStudiesTrials
Chronic Primary Open Angle Glaucoma
[description not available]		04.821
Glaucoma, Suspect
[description not available]		05.732
Glaucoma, Open-Angle
Glaucoma in which the angle of the anterior chamber is open and the trabecular meshwork does not encroach on the base of the iris.		04.821
Intraocular Pressure
The pressure of the fluids in the eye.		011.4453
Ocular Hypertension
A condition in which the intraocular pressure is elevated above normal and which may lead to glaucoma.		17.732
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.1310
Autoimmune Disease
[description not available]		03.2310
Autoimmune Diseases
Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.		03.2310
Glaucoma
An ocular disease, occurring in many forms, having as its primary characteristics an unstable or a sustained increase in the intraocular pressure which the eye cannot withstand without damage to its structure or impairment of its function. The consequences of the increased pressure may be manifested in a variety of symptoms, depending upon type and severity, such as excavation of the optic disk, hardness of the eyeball, corneal anesthesia, reduced visual acuity, seeing of colored halos around lights, disturbed dark adaptation, visual field defects, and headaches. (Dictionary of Visual Science, 4th ed)		111.0221
Exfoliation Glaucoma
[description not available]		03.5111
Exfoliation Syndrome
The deposition of flaky, translucent fibrillar material most conspicuous on the anterior lens capsule and pupillary margin but also in both surfaces of the iris, the zonules, trabecular meshwork, ciliary body, corneal endothelium, and orbital blood vessels. It sometimes forms a membrane on the anterior iris surface. Exfoliation refers to the shedding of pigment by the iris. (Newell, Ophthalmology, 7th ed, p380)		08.5111