Compounds > rki-1447
Page last updated: 2024-11-13

rki-1447

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Description

RKI-1447: an antineoplastic agent that inhibits ROCK1 and ROCK2; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60138149
CHEMBL ID3218011
SCHEMBL ID2560201
MeSH IDM0579808

Synonyms (42)

Synonym
1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea
07r ,
3TWJ
S7195
CHEMBL3218011
1-[(3-hydroxyphenyl)methyl]-3-[4-(pyridin-4-yl)-1,3-thiazol-2-yl]urea
gtpl8152
compound 5g [pmid 23275831]
1342278-01-6
rki-1447
FD5032 ,
HY-15755
CS-1632
1-(3-hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea
SCHEMBL2560201
rki1447
rki 1447
AC-32843
AKOS025405230
EX-A238
HMS3653E17
us9221808, 1bo-mes
bdbm199250
us9221808, 1bo
us9221808, 1bo-hcl
NCGC00371153-09
SW219877-1
FT-0700170
BCP08076
mfcd26142658
Q27088558
SB19472
CCG-267765
A887942
AS-55958
NCGC00371153-01
urea, n-((3-hydroxyphenyl)methyl)-n'-(4-(4-pyridinyl)-2-thiazolyl)-
f8gz6c9mkz ,
unii-f8gz6c9mkz
n-((3-hydroxyphenyl)methyl)-n'-(4-(4-pyridinyl)-2-thiazolyl)urea
BR172011
DTXSID501336679

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency18.55690.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.53550.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency0.30110.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency0.84870.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency13.99300.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency0.30110.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency0.30110.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency0.30110.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Rho-associated protein kinase 2Homo sapiens (human)IC50 (µMol)0.00610.00020.578010.0000AID1119754; AID1846050
Rho-associated protein kinase 1Homo sapiens (human)IC50 (µMol)0.01120.00040.854910.0000AID1119753; AID1846049
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (130)

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)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo 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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

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)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo 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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

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)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo 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)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (19)

Assay IDTitleYearJournalArticle
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2012Cancer research, Oct-01, Volume: 72, Issue:19
RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1119753Inhibition of N-terminal GST-tagged ROCK1 (1 to 535) (unknown origin) using KKRPQRRSNVF as substrate after 1 hr by Z-Lyte-based FRET assay2012MedChemComm, Jun-01, Volume: 3, Issue:6
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
AID1846049Inhibition of ROCK1 (unknown origin)2021European journal of medicinal chemistry, Apr-05, Volume: 215Medulloblastoma drugs in development: Current leads, trials and drawbacks.
AID1119754Inhibition of N-terminal GST-tagged ROCK2 (1 to 552) (unknown origin) using KKRPQRRSNVF as substrate after 1 hr by Z-Lyte-based FRET assay2012MedChemComm, Jun-01, Volume: 3, Issue:6
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
AID1846050Inhibition of ROCK2 (unknown origin)2021European journal of medicinal chemistry, Apr-05, Volume: 215Medulloblastoma drugs in development: Current leads, trials and drawbacks.
AID1345316Human Rho associated coiled-coil containing protein kinase 1 (Rho kinase)2012MedChemComm, Jun-01, Volume: 3, Issue:6
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
AID1345327Human Rho associated coiled-coil containing protein kinase 2 (Rho kinase)2012MedChemComm, Jun-01, Volume: 3, Issue:6
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
AID1345768Human LIM domain kinase 1 (LIMK subfamily)2012MedChemComm, Jun-01, Volume: 3, Issue:6
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
AID1345761Human p21 (RAC1) activated kinase 1 (PAKA subfamily)2012MedChemComm, Jun-01, Volume: 3, Issue:6
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
AID1345312Human CDC42 binding protein kinase alpha (GEK subfamily)2012MedChemComm, Jun-01, Volume: 3, Issue:6
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
AID1345365Human protein kinase N1 (Protein kinase N (PKN) family)2012MedChemComm, Jun-01, Volume: 3, Issue:6
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
AID1345342Human myosin light chain kinase (Myosin Light Chain Kinase (MLCK) family)2012MedChemComm, Jun-01, Volume: 3, Issue:6
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
AID1345375Human DM1 protein kinase (GEK subfamily)2012MedChemComm, Jun-01, Volume: 3, Issue:6
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

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 (36.36)24.3611
2020's7 (63.64)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.39

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 Index21.39 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.39)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (9.09%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (90.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		3.2850isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
fasudil
fasudil: intracellular calcium antagonist; structure in first source. fasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia.		2.0710isoquinolines;
N-sulfonyldiazepane		antihypertensive agent;
calcium channel blocker;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
geroprotector;
neuroprotective agent;
nootropic agent;
vasodilator agent
mebendazole
Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5.		3.4110aromatic ketone;
benzimidazoles;
carbamate ester		antinematodal drug;
microtubule-destabilising agent;
tubulin modulator
thiazoles
[no description available]		3.28501,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
malondialdehyde
Malondialdehyde: The dialdehyde of malonic acid.. malonaldehyde : A dialdehyde that is propane substituted by two oxo groups at the terminal carbon atoms respectively. A biomarker of oxidative damage to lipids caused by smoking, it exists in vivo mainly in the enol form.		2.2510dialdehydebiomarker
fingolimod
fingolimod : An aminodiol that consists of propane-1,3-diol having amino and 2-(4-octylphenyl)ethyl substituents at the 2-position. It is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. A prodrug, fingolimod is phosphorylated by sphingosine kinase to active metabolite fingolimod-phosphate, a structural analogue of sphingosine 1-phosphate.		3.4110aminodiol;
primary amino compound		antineoplastic agent;
CB1 receptor antagonist;
immunosuppressive agent;
prodrug;
sphingosine-1-phosphate receptor agonist
arsenic trioxide
[no description available]		3.4110
oleic acid
Oleic Acid: An unsaturated fatty acid that is the most widely distributed and abundant fatty acid in nature. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. (Stedman, 26th ed). oleic acid : An octadec-9-enoic acid in which the double bond at C-9 has Z (cis) stereochemistry.		7.2510octadec-9-enoic acidantioxidant;
Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
Escherichia coli metabolite;
mouse metabolite;
plant metabolite;
solvent
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.		2.0710aromatic amide
tolfenamic acid
tolfenamic acid: structure. tolfenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 3-chloro-2-methylphenyl group. Tolfenamic acid is used specifically for relieving the pain of migraine. It also shows anticancer activity.		3.4110aminobenzoic acid;
organochlorine compound;
secondary amino compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
s 1033
[no description available]		3.4110(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
digoxin
Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.		3.4110cardenolide glycoside;
steroid saponin		anti-arrhythmia drug;
cardiotonic drug;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
epitope
pyrvinium
pyrvinium: RN given refers to parent cpd; synonyms vanquin & vankin refer to pamoate[2:1]; structure in Merck Index, 9th ed, #7810. pyrvinium : A quinolinium ion that is 1-methylquinolinium substituted by dimethylamino group at position 6 and a (E)-2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)ethenyl at position 2. It is a anthelminthic drug active against pinworms. The salts of pyrvinium can also be used as anticancer agents.		3.4110quinolinium ionanthelminthic drug;
antineoplastic agent
fenretinide
Fenretinide: A synthetic retinoid that is used orally as a chemopreventive against prostate cancer and in women at risk of developing contralateral breast cancer. It is also effective as an antineoplastic agent.. 4-hydroxyphenyl retinamide : A retinoid obtained by formal condensation of the carboxy group of all-trans retinoic acid and the anilino group of 4-hydroxyaniline. Synthetic retinoid agonist. Antiproliferative, antioxidant and anticancer agent with a long half-life in vivo. Apoptotic effects appear to be mediated by a mechanism distinct from that of 'classical' retinoids.		3.4110monocarboxylic acid amide;
retinoid		antineoplastic agent;
antioxidant
palbociclib
[no description available]		3.4110aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
laq824
LAQ824: Histone deacetylase inhibitor		3.4110
panobinostat
Panobinostat: An indole and hydroxamic acid derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used as an antineoplastic agent in combination with BORTEZOMIB and DEXAMETHASONE for the treatment of MULTIPLE MYELOMA.. panobinostat : A hydroxamic acid obtained by formal condensation of the carboxy group of (2E)-3-[4-({[2-(2-methylindol-3-yl)ethyl]amino}methyl)phenyl]prop-2-enoic acid with the amino group of hydroxylamine. A histone deacetylase inhibitor used (as its lactate salt) in combination with bortezomib and dexamethasone for the treatment of multiple myeloma.		3.4110cinnamamides;
hydroxamic acid;
methylindole;
secondary amino compound		angiogenesis modulating agent;
antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor
6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)-
[no description available]		3.4110organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
aee 788
AEE 788: structure in first source		3.41106-{4-[(4-ethylpiperazin-1-yl)methyl]phenyl}-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amineangiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist;
trypanocidal drug
quisinostat
[no description available]		3.4110indoles
buparlisib
NVP-BKM120: a pan class I PI3 kinase inhibitor with antineoplastic activity; structure in first source		3.4110aminopyridine;
aminopyrimidine;
morpholines;
organofluorine compound		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
pha 848125
N,1,4,4-tetramethyl-8-((4-(4-methylpiperazin-1-yl)phenyl)amino)-4,5-dihydro-1H-pyrazolo(4,3-h)quinazoline-3-carboxamide: a cyclin dependent kinase inhibitor		3.4110
cx 4945
[no description available]		3.4110
mk-1775
adavosertib: a Wee1 kinase inhibitor; structure in first source		3.4110piperazines
gsk 1363089
GSK 1363089: a multikinase inhibitor that acts on Met, RON, Axl, and VEGFR; structure in first source		3.4110aromatic ether
tak-441
TAK-441: structure in first source		3.4110
jq1 compound
[no description available]		3.4110carboxylic ester;
organochlorine compound;
tert-butyl ester;
thienotriazolodiazepine		angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
bromodomain-containing protein 4 inhibitor;
cardioprotective agent;
ferroptosis inducer
ly2940680
[no description available]		3.4110
gsk1210151a
GSK1210151A: inhibitor of the BET family of proteins; structure in first source		3.4110imidazoquinoline
pf-5274857
1-(4-(5'-chloro-3,5-dimethyl-2,4'-bipyridin-2'-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one: a potent and selective Smoothened antagonist that penetrates the blood-brain barrier; structure in first source		3.4110
ConditionIndicatedRelationship StrengthStudiesTrials
Breast Cancer
[description not available]		07.0710
Experimental Mammary Neoplasms
[description not available]		02.0710
Invasiveness, Neoplasm
[description not available]		02.5320
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.0710
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.9330
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Benign Cerebellar Neoplasms
[description not available]		03.2310
Arachnoidal Cerebellar Sarcoma, Circumscribed
[description not available]		03.2310
Medulloblastoma
A malignant neoplasm that may be classified either as a glioma or as a primitive neuroectodermal tumor of childhood (see NEUROECTODERMAL TUMOR, PRIMITIVE). The tumor occurs most frequently in the first decade of life with the most typical location being the cerebellar vermis. Histologic features include a high degree of cellularity, frequent mitotic figures, and a tendency for the cells to organize into sheets or form rosettes. Medulloblastoma have a high propensity to spread throughout the craniospinal intradural axis. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2060-1)		03.2310
Degenerative Disc Disease
[description not available]		02.3110
Intervertebral Disc Degeneration
Degenerative changes in the INTERVERTEBRAL DISC due to aging or structural damage, especially to the vertebral end-plates.		02.3110
Fatty Liver, Nonalcoholic
[description not available]		02.2510
Hepatocellular Carcinoma
[description not available]		07.2510
Insulin Sensitivity
[description not available]		02.2510
Cancer of Liver
[description not available]		02.2510
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		02.2510
Insulin Resistance
Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.		02.2510
Liver Neoplasms
Tumors or cancer of the LIVER.		02.2510
Non-alcoholic Fatty Liver Disease
Fatty liver finding without excessive ALCOHOL CONSUMPTION.		07.2510
Chronic Primary Open Angle Glaucoma
[description not available]		02.2110
Ocular Hypotension
Abnormally low intraocular pressure often related to chronic inflammation (uveitis).		07.2110
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.		02.2110
Intraocular Pressure
The pressure of the fluids in the eye.		02.2110
Colorectal Cancer
[description not available]		02.2510
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		02.2510