Page last updated: 2024-12-05

strophanthidin

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Description

Strophanthidin: 3 beta,5,14-Trihydroxy-19-oxo-5 beta-card-20(22)-enolide. The aglycone cardioactive agent isolated from Strophanthus Kombe, S. gratus and other species; it is a very toxic material formerly used as digitalis. Synonyms: Apocymarin; Corchorin; Cynotoxin; Corchorgenin. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
StrophanthusgenusA plant genus of the family APOCYNACEAE that contains OUABAIN cardiac glycosides.[MeSH]ApocynaceaeThe dogbane family of the order Gentianales. Members of the family have milky, often poisonous juice, smooth-margined leaves, and flowers in clusters.[MeSH]
Strophanthus kombespecies[no description available]ApocynaceaeThe dogbane family of the order Gentianales. Members of the family have milky, often poisonous juice, smooth-margined leaves, and flowers in clusters.[MeSH]

Cross-References

ID SourceID
PubMed CID6185
CHEMBL ID111743
CHEBI ID38178
SCHEMBL ID240582
MeSH IDM0020622

Synonyms (86)

Synonym
smr001233308
MLS002153969 ,
BRD-K84595254-001-03-0
NCI60_041903
3-beta,5,14-trioxy-19-oxo-carden-(20:22)-olid [german]
einecs 200-626-6
5beta-card-20(22)-enolide, 3beta,5,14-trihydroxy-19-oxo-
(3beta,5beta)-3,5,14-trihydroxy-19-oxocard-20(22)-enolide
3-beta,5,14-trihydroxy-19-oxo-5-beta-card-20(22)-enolide
brn 0097859
5-beta-hydroxy-19-oxodigitoxigenin
card-20(22)-enolide, 3,5,14-trihydroxy-19-oxo-, (3-beta,5-beta)-
19-oxo-cardogenen-(20:22)-triol-(3-beta,5,14) [german]
nsc 86078
5-beta-card-20(22)-enolide, 3-beta,5,14-trihydroxy-19-oxo-
3-beta,5,14-trioxy-19-oxo-digen-(20:22)-olid [german]
CHEBI:38178 ,
5beta-hydroxy-19-oxodigitoxigenin
3beta,5,14-trihydroxy-19-oxo-5beta-card-20(22)-enolide
strophanthidin k
BPBIO1_000989
PRESTWICK_117
PRESTWICK2_000710
strophanthidine
NSC86078 ,
apocynamarin
strophanthidin
(3.beta.,5.beta.)-3,5,14-trihydroxy-19-oxocard-20(22)-enolide
(3s,5s,8r,9s,10s,13r,14s,17r)-3,5,14-trihydroxy-13-methyl-17-(5-oxo-2h-furan-3-yl)-2,3,4,6,7,8,9,11,12,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthrene-10-carbaldehyde
convallatoxigenin
kappa-strophanthidine
66-28-4
wln: l e5 b666tj avh e1 iq mq oq f- dt5ov ehj
3.beta.,14-trihydroxy-19-oxo-5.beta.-card-20(22)-enolide
corchsularin
k-strophanthidine
corchoside a, aglycon
erysimupikron
nsc-86078
card-20(22)-enolide,5,14-trihydroxy-19-oxo-, (3.beta.,5.beta.)-
corchorin
5.beta.-card-20(22)-enolide,5,14-trihydroxy-19-oxo-
corchoside a aglycon
cymarigenin
cynotoxin
erysimupicrone
k-strophanthidin
corchorgenin
PRESTWICK3_000710
BSPBIO_000899
PRESTWICK0_000710
SPBIO_002820
PRESTWICK1_000710
NCGC00142399-02
CHEMBL111743
HMS1570M21
LMST01120005
HMS2097M21
card-20(22)-enolide, 3,5,14-trihydroxy-19-oxo-, (3beta,5beta)-
3-beta,5,14-trioxy-19-oxo-digen-(20:22)-olid
3-beta,5,14-trioxy-19-oxo-carden-(20:22)-olid
unii-w5o632dn33
apocymarin
19-oxo-cardogenen-(20:22)-triol-(3-beta,5,14)
w5o632dn33 ,
5-18-05-00126 (beilstein handbook reference)
C19988
HMS2233O14
(1s,2s,5s,7s,11s,10r,14r,15r)-5,7,11-trihydroxy-15-methyl-14-(5-oxo(3-2-hydrof uryl))tetracyclo[8.7.0.0<2,7>.0<11,15>]heptadecane-2-carbaldehyde
strophanthin-k [who-dd]
strophanthidin [mi]
card-20(22)-enolide, 3,5,14-trihydroxy-19-oxo-
strophanthin-k
SCHEMBL240582
ODJLBQGVINUMMR-HZXDTFASSA-N
AKOS024280415
SR-01000838893-2
sr-01000838893
DTXSID00903966
Q1718068
BRD-K84595254-001-10-5
strophantidin
bdbm50255120
F82324
HY-114252
CS-0080731

Research Excerpts

Effects

ExcerptReferenceRelevance
"Strophanthidin has no demonstrable effect on membrane conductance apart from that due to the observed depolarization."( Contribution of sodium pump to resting potential of squid giant axon.
de Weer, P; Geduldig, D, 1978
)
0.98

Actions

ExcerptReferenceRelevance
"Strophanthidin caused an increase in contractile force ("therapeutic effect") followed by a subsequent decrease and by the onset of arrhythmias ("toxic effects")."( Effect of calcium on strophanthidin-induced electrical and mechanical toxicity in cardiac Purkinje fibers.
Lin, CI; Vassalle, M, 1979
)
1.3

Toxicity

We used Na(+)-sensitive microelectrodes to measure changes in intracellular Na+ activity (aiNa) associated with positive inotropic and toxic effects. The tendency of a given oral dose of digoxin to induce cardiac dysrhythmia was determined indirectly at various times after its administration to eight conscious dogs.

ExcerptReferenceRelevance
"1 The tendency of a given oral dose of digoxin to induce cardiac dysrhythmia was determined indirectly at various times after its administration to eight conscious dogs by measurement of the intravenous dose of acetylstrophanthidin necessary to induce toxic changes in the ECG."( The relationship between cardiotoxicity and plasma digoxin concentration in conscious dogs.
Chapple, DJ; Hughes, R; Johnson, BF, 1976
)
0.44
" We used Na(+)-sensitive microelectrodes to measure changes in intracellular Na+ activity (aiNa) associated with positive inotropic and toxic effects of acetylstrophanthidin (AS) and a semisynthetic agent, actodigin."( Effects of different cardiac steroids on intracellular sodium, inotropy and toxicity in sheep Purkinje fibers.
Farkas, DE; Norell, MA; Vereault, DV; Wasserstrom, JA, 1991
)
0.48
"In the in vitro perfusion of the isolated heart, toxic doses of cardiac glycosides produce an inotropic response which is followed by a decline in contractile force and an increase in the resting tension."( Digitalis-induced mechanical toxicity: protection by slow Ca++ channel blockers.
Agbanyo, M; Bains, R; Hoeschen, RJ; Khatter, JC; Navaratnam, S, 1986
)
0.27

Compound-Compound Interactions

ExcerptReferenceRelevance
" Selected cardiac glycosides were tested in combination with four clinically relevant cytotoxic drugs (5-fluorouracil, oxaliplatin, cisplatin, irinotecan)."( Cytotoxic effects of cardiac glycosides in colon cancer cells, alone and in combination with standard chemotherapeutic drugs.
Bohlin, L; Felth, J; Fryknäs, M; Gullbo, J; Lindskog, M; Rickardson, L; Rosén, J; Wickström, M, 2009
)
0.35

Dosage Studied

There was no correlation between plasma levels of digoxin and the tendency to dysrhythmia. maximal sensitivity to acetylstrophanthidin was found 3 to 6 h after administration ofDigoxin. No apparent right or left shift in dose-response curve for the positive inotropic effect of strophanthidin.

ExcerptRelevanceReference
" The rates of such an increase were measured during this period at various cardioactive steroid concentrations and used to produce dose-response curves."( The intracellular sodium activity of cardiac Purkinje fibres during inhibition and re-activation of the Na-K pump.
Deitmer, JW; Ellis, D, 1978
)
0.26
" In that way of dose-response curves for the rapid effects of ouabain and other inhibitors of active Na transport were obtained with both the original, ouabain-sensitive (OS) and the variant, ouabain-resistant (OR) cells."( Variant HeLa cells selected for their resistance to ouabain.
Rosenberg, HM, 1975
)
0.25
" Whereas contractility increased in response to small doses of digitalis, displaying a linear dose-response relation independent of autonomic tone, A-V nodal transmission indexes responded minimally to less than 50 percent of the toxic dose of digitalis, and the response was dependent upon autonomic tone."( Dissociation of the inotropic effect of digitalis from its effect on atrioventricular conduction.
Kim, YI; Noble, RJ; Zipes, DP, 1975
)
0.25
" 4 There was no correlation between plasma levels of digoxin and the tendency to dysrhythmia, since peak plasma concentrations of digoxin were reached at about 60 min after dosing whereas maximal sensitivity to acetylstrophanthidin was found 3 to 6 h after administration of digoxin."( The relationship between cardiotoxicity and plasma digoxin concentration in conscious dogs.
Chapple, DJ; Hughes, R; Johnson, BF, 1976
)
0.44
" The dose-response relationship to Str in four oocytes displayed a mean K0."( Voltage dependence of current through the Na,K-exchange pump of Rana oocytes.
Civan, MM; Wu, MM, 1991
)
0.28
" No apparent right or left shift in dose-response curve for the positive inotropic effect of strophanthidin was observed and toxic concentrations of strophanthidin were unchanged; however, the degree of the positive inotropic effect produced by high concentrations of strophanthidin was significantly smaller in hypertrophied muscle."( Pressure-induced cardiac hypertrophy: changes in Na+,K+-ATPase and glycoside actions in cats.
Akera, T; Nirasawa, Y, 1987
)
0.49
" The differences between the dose-response curve of glibenclamide and those of tolbutamide or carbutamide were significant."( The effect of various hypoglycaemic sulphonylureas on the cardiotoxicity of glycosides and arrhythmogenic activity due to myocardial ischaemia.
Balkányi, I; Dévai, I; Kiss, V; Koltai, MZ; Köszeghy, A; Pogátsa, G, 1988
)
0.27
" Dose-response curves plotted as percentage change from baseline versus concentration of drug were determined for acetylstrophanthidin, isoproterenol, isobutylmethylxanthine, and milrinone."( Decreased inotropic but relatively preserved relaxation response to cyclic adenosine monophosphate-dependent agents in myopathic human myocardium.
Bruce, E; Flemmal, K; Grossman, W; Gutstein, DE; Gwathmey, JK; Markis, JE; Morgan, JP; Ransil, BJ; Travers, KE, 1996
)
0.5
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (6)

ClassDescription
3beta-hydroxy steroidA 3-hydroxy steroid in which the 3-hydroxy substituent is in the beta-position.
14beta-hydroxy steroidA 14-hydroxy steroid in which the hydroxy group has a beta-configuration.
5beta-hydroxy steroid
19-oxo steroid
cardenolidesAny steroid lactone that is a C23 steroid with a five-membered lactone ring at C-17 and its substituted derivatives. They form the aglycone constituents of cardiac glycosides.
steroid aldehydeAny steroid substituted by a formyl group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glp-1 receptor, partialHomo sapiens (human)Potency1.00000.01846.806014.1254AID624417
BRCA1Homo sapiens (human)Potency1.25890.89137.722525.1189AID624202
ATAD5 protein, partialHomo sapiens (human)Potency0.99640.004110.890331.5287AID504466; AID504467
TDP1 proteinHomo sapiens (human)Potency6.24060.000811.382244.6684AID686978; AID686979
TSHR proteinHomo sapiens (human)Potency0.84920.338119.046637.9330AID602292
Smad3Homo sapiens (human)Potency7.07950.00527.809829.0929AID588855
67.9K proteinVaccinia virusPotency1.00000.00018.4406100.0000AID720579; AID720580
IDH1Homo sapiens (human)Potency1.15820.005210.865235.4813AID686970
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency1.77830.01262.451825.0177AID485313
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency0.33510.00419.984825.9290AID504444; AID720524
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency50.11870.794321.275750.1187AID624246
ras-related protein Rab-9AHomo sapiens (human)Potency1.41250.00022.621531.4954AID485297
gemininHomo sapiens (human)Potency1.45970.004611.374133.4983AID624296; AID624297
[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)
Sodium/potassium-transporting ATPase subunit beta-1 Rattus norvegicus (Norway rat)IC50 (µMol)0.00240.00240.64654.3000AID1455007
Sodium/potassium-transporting ATPase subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.00240.00180.00520.0120AID1455007
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Hypoxia-inducible factor 1-alphaHomo sapiens (human)EC50 (µMol)2.00000.02001.29905.0100AID421968
Endothelial PAS domain-containing protein 1Homo sapiens (human)EC50 (µMol)2.00000.02000.93303.3000AID421968
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PAX8Homo sapiens (human)AC501.24000.04885.435469.1700AID687027; AID687029
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (98)

Processvia Protein(s)Taxonomy
positive regulation of chemokine-mediated signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of signaling receptor activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to hypoxiaHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of DNA-templated transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to reactive oxygen speciesHypoxia-inducible factor 1-alphaHomo sapiens (human)
angiogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to hypoxiaHypoxia-inducible factor 1-alphaHomo sapiens (human)
intracellular glucose homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
neural crest cell migrationHypoxia-inducible factor 1-alphaHomo sapiens (human)
epithelial to mesenchymal transitionHypoxia-inducible factor 1-alphaHomo sapiens (human)
embryonic placenta developmentHypoxia-inducible factor 1-alphaHomo sapiens (human)
B-1 B cell homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of endothelial cell proliferationHypoxia-inducible factor 1-alphaHomo sapiens (human)
heart loopingHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of neuroblast proliferationHypoxia-inducible factor 1-alphaHomo sapiens (human)
chondrocyte differentiationHypoxia-inducible factor 1-alphaHomo sapiens (human)
glandular epithelial cell maturationHypoxia-inducible factor 1-alphaHomo sapiens (human)
connective tissue replacement involved in inflammatory response wound healingHypoxia-inducible factor 1-alphaHomo sapiens (human)
outflow tract morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
cardiac ventricle morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
lactate metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of glycolytic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of DNA-templated transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
intracellular iron ion homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
signal transductionHypoxia-inducible factor 1-alphaHomo sapiens (human)
neuroblast proliferationHypoxia-inducible factor 1-alphaHomo sapiens (human)
lactationHypoxia-inducible factor 1-alphaHomo sapiens (human)
visual learningHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to iron ionHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of gene expressionHypoxia-inducible factor 1-alphaHomo sapiens (human)
vascular endothelial growth factor productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of gene expressionHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of gene expressionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of epithelial cell migrationHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to muscle activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
axonal transport of mitochondrionHypoxia-inducible factor 1-alphaHomo sapiens (human)
neural fold elevation formationHypoxia-inducible factor 1-alphaHomo sapiens (human)
cerebral cortex developmentHypoxia-inducible factor 1-alphaHomo sapiens (human)
bone mineralizationHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of bone mineralizationHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
TOR signalingHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of TOR signalingHypoxia-inducible factor 1-alphaHomo sapiens (human)
intracellular oxygen homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of chemokine productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of transforming growth factor beta2 productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
collagen metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to oxidative stressHypoxia-inducible factor 1-alphaHomo sapiens (human)
embryonic hemopoiesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
insulin secretion involved in cellular response to glucose stimulusHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusHypoxia-inducible factor 1-alphaHomo sapiens (human)
hemoglobin biosynthetic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of erythrocyte differentiationHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of angiogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of growthHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHypoxia-inducible factor 1-alphaHomo sapiens (human)
muscle cell cellular homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of hormone biosynthetic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
digestive tract morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of nitric-oxide synthase activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
neuron apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
elastin metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
intestinal epithelial cell maturationHypoxia-inducible factor 1-alphaHomo sapiens (human)
epithelial cell differentiation involved in mammary gland alveolus developmentHypoxia-inducible factor 1-alphaHomo sapiens (human)
iris morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
retina vasculature development in camera-type eyeHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of thymocyte apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to interleukin-1Hypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to hypoxiaHypoxia-inducible factor 1-alphaHomo sapiens (human)
dopaminergic neuron differentiationHypoxia-inducible factor 1-alphaHomo sapiens (human)
mesenchymal cell apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
hypoxia-inducible factor-1alpha signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to virusHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of cytokine production involved in inflammatory responseHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of mitophagyHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of miRNA transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of miRNA transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of aerobic respirationHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of reactive oxygen species metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of protein neddylationHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of mesenchymal cell apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of transcription by RNA polymerase IIHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to hypoxiaEndothelial PAS domain-containing protein 1Homo sapiens (human)
angiogenesisEndothelial PAS domain-containing protein 1Homo sapiens (human)
embryonic placenta developmentEndothelial PAS domain-containing protein 1Homo sapiens (human)
blood vessel remodelingEndothelial PAS domain-containing protein 1Homo sapiens (human)
regulation of heart rateEndothelial PAS domain-containing protein 1Homo sapiens (human)
epithelial cell maturationEndothelial PAS domain-containing protein 1Homo sapiens (human)
response to oxidative stressEndothelial PAS domain-containing protein 1Homo sapiens (human)
mitochondrion organizationEndothelial PAS domain-containing protein 1Homo sapiens (human)
signal transductionEndothelial PAS domain-containing protein 1Homo sapiens (human)
visual perceptionEndothelial PAS domain-containing protein 1Homo sapiens (human)
erythrocyte differentiationEndothelial PAS domain-containing protein 1Homo sapiens (human)
lung developmentEndothelial PAS domain-containing protein 1Homo sapiens (human)
norepinephrine metabolic processEndothelial PAS domain-containing protein 1Homo sapiens (human)
mRNA transcription by RNA polymerase IIEndothelial PAS domain-containing protein 1Homo sapiens (human)
surfactant homeostasisEndothelial PAS domain-containing protein 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIEndothelial PAS domain-containing protein 1Homo sapiens (human)
myoblast fate commitmentEndothelial PAS domain-containing protein 1Homo sapiens (human)
multicellular organismal-level iron ion homeostasisEndothelial PAS domain-containing protein 1Homo sapiens (human)
cellular response to hypoxiaEndothelial PAS domain-containing protein 1Homo sapiens (human)
positive regulation of cold-induced thermogenesisEndothelial PAS domain-containing protein 1Homo sapiens (human)
regulation of protein neddylationEndothelial PAS domain-containing protein 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIEndothelial PAS domain-containing protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
DNA-binding transcription factor activity, RNA polymerase II-specificHypoxia-inducible factor 1-alphaHomo sapiens (human)
sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificHypoxia-inducible factor 1-alphaHomo sapiens (human)
cis-regulatory region sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription activator activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription repressor activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
transcription coactivator bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificHypoxia-inducible factor 1-alphaHomo sapiens (human)
p53 bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription factor activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
nuclear receptor bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
enzyme bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein kinase bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein domain specific bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
ubiquitin protein ligase bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
histone deacetylase bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein heterodimerization activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
Hsp90 protein bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
E-box bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
transcription regulator activator activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
sequence-specific DNA bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEndothelial PAS domain-containing protein 1Homo sapiens (human)
transcription coactivator bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificEndothelial PAS domain-containing protein 1Homo sapiens (human)
protein bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
protein heterodimerization activityEndothelial PAS domain-containing protein 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingEndothelial PAS domain-containing protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
nucleusHypoxia-inducible factor 1-alphaHomo sapiens (human)
nucleoplasmHypoxia-inducible factor 1-alphaHomo sapiens (human)
cytoplasmHypoxia-inducible factor 1-alphaHomo sapiens (human)
cytosolHypoxia-inducible factor 1-alphaHomo sapiens (human)
nuclear bodyHypoxia-inducible factor 1-alphaHomo sapiens (human)
nuclear speckHypoxia-inducible factor 1-alphaHomo sapiens (human)
motile ciliumHypoxia-inducible factor 1-alphaHomo sapiens (human)
axon cytoplasmHypoxia-inducible factor 1-alphaHomo sapiens (human)
chromatinHypoxia-inducible factor 1-alphaHomo sapiens (human)
euchromatinHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein-containing complexHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexHypoxia-inducible factor 1-alphaHomo sapiens (human)
nucleoplasmEndothelial PAS domain-containing protein 1Homo sapiens (human)
cytosolEndothelial PAS domain-containing protein 1Homo sapiens (human)
nuclear speckEndothelial PAS domain-containing protein 1Homo sapiens (human)
chromatinEndothelial PAS domain-containing protein 1Homo sapiens (human)
transcription regulator complexEndothelial PAS domain-containing protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (51)

Assay IDTitleYearJournalArticle
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1072834Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Cytotoxic cardiac glycosides and coumarins from Antiaris toxicaria.
AID492115Cardiotonic activity in guinea pig right ventricular muscles assessed as minimum positive inotropic effective concentration causing myocardial contraction2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Cardiac glycosides from Antiaris toxicaria with potent cardiotonic activity.
AID77697Inotropic activity on cardiac frequency on spontaneously beating guinea pig right atria, (from basal frequency).2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Inotropic activity of hydroindene amidinohydrazones.
AID1072827Cytotoxicity against human CAKI-1 cells assessed as growth inhibition after 72 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Cytotoxic cardiac glycosides and coumarins from Antiaris toxicaria.
AID421971Growth inhibition of human U251 cells stably transfected with pGL3 plasmid after 24 hrs2009Journal of natural products, May-22, Volume: 72, Issue:5
Cytotoxic and HIF-1alpha inhibitory compounds from Crossosoma bigelovii.
AID1072826Cytotoxicity against human HCT9 cells assessed as growth inhibition after 72 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Cytotoxic cardiac glycosides and coumarins from Antiaris toxicaria.
AID471510Cytotoxicity against human HT-29 cells assessed as survival index at 10 uM after 72 hrs by FMCA method2009Journal of natural products, Nov, Volume: 72, Issue:11
Cytotoxic effects of cardiac glycosides in colon cancer cells, alone and in combination with standard chemotherapeutic drugs.
AID492116Cardiotonic activity in guinea pig left atrial muscles assessed as maximum positive inotropic effective concentration causing myocardial contraction relative to basal level2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Cardiac glycosides from Antiaris toxicaria with potent cardiotonic activity.
AID127349Binding affinity against human monoclonal antibody (mAb)-11E62002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Three-dimensional quantitative structure-activity relationship analysis of ligand binding to human sequence antidigoxin monoclonal antibodies using comparative molecular field analysis.
AID127351Binding affinity against human monoclonal antibody (mAb)-5C22002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Three-dimensional quantitative structure-activity relationship analysis of ligand binding to human sequence antidigoxin monoclonal antibodies using comparative molecular field analysis.
AID1072829Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Cytotoxic cardiac glycosides and coumarins from Antiaris toxicaria.
AID492117Cardiotonic activity in guinea pig right ventricular muscles assessed as maximum positive inotropic effective concentration causing myocardial contraction relative to basal level2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Cardiac glycosides from Antiaris toxicaria with potent cardiotonic activity.
AID400010Cytotoxicity against human KB cells
AID492119Safety index, ratio of arrhythmogenic concentration to minimum positive inotropic effective concentration causing myocardial contraction in guinea pig right ventricular muscles2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Cardiac glycosides from Antiaris toxicaria with potent cardiotonic activity.
AID1072830Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Cytotoxic cardiac glycosides and coumarins from Antiaris toxicaria.
AID77699Inotropic activity on electrically driven isolated Guinea pig left atria, (from basal force).2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Inotropic activity of hydroindene amidinohydrazones.
AID421968Inhibition of HIF1 activation in human U251 cells stably transfected in pGL2-TK-HRE plasmid under hypoxic condition after 16 to 24 hrs by luciferase reporter gene assay2009Journal of natural products, May-22, Volume: 72, Issue:5
Cytotoxic and HIF-1alpha inhibitory compounds from Crossosoma bigelovii.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID127350Binding affinity against human monoclonal antibody (mAb)-1B32002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Three-dimensional quantitative structure-activity relationship analysis of ligand binding to human sequence antidigoxin monoclonal antibodies using comparative molecular field analysis.
AID421969Inhibition of HIF1 activation in human U251 cells stably transfected in pGL3 plasmid under hypoxic condition after 16 to 24 hrs by luciferase reporter gene assay2009Journal of natural products, May-22, Volume: 72, Issue:5
Cytotoxic and HIF-1alpha inhibitory compounds from Crossosoma bigelovii.
AID421970Growth inhibition of human U251 cells stably transfected with pGL2-TK-HRE plasmid after 24 hrs2009Journal of natural products, May-22, Volume: 72, Issue:5
Cytotoxic and HIF-1alpha inhibitory compounds from Crossosoma bigelovii.
AID1072832Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Cytotoxic cardiac glycosides and coumarins from Antiaris toxicaria.
AID1072828Cytotoxicity against human 1A9 cells assessed as growth inhibition after 72 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Cytotoxic cardiac glycosides and coumarins from Antiaris toxicaria.
AID471508Cytotoxicity against human CC20 cells assessed as survival index at 10 uM after 72 hrs by FMCA method2009Journal of natural products, Nov, Volume: 72, Issue:11
Cytotoxic effects of cardiac glycosides in colon cancer cells, alone and in combination with standard chemotherapeutic drugs.
AID127479Binding affinity against murine monoclonal antibody (mAb)-40-502002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Three-dimensional quantitative structure-activity relationship analysis of ligand binding to human sequence antidigoxin monoclonal antibodies using comparative molecular field analysis.
AID1072833Cytotoxicity against human KBVIN cells assessed as growth inhibition after 72 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Cytotoxic cardiac glycosides and coumarins from Antiaris toxicaria.
AID492114Cardiotonic activity in guinea pig left atrial muscles assessed as minimum positive inotropic effective concentration causing myocardial contraction2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Cardiac glycosides from Antiaris toxicaria with potent cardiotonic activity.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID471509Cytotoxicity against human HCT116 cells assessed as survival index at 10 uM after 72 hrs by FMCA method2009Journal of natural products, Nov, Volume: 72, Issue:11
Cytotoxic effects of cardiac glycosides in colon cancer cells, alone and in combination with standard chemotherapeutic drugs.
AID492118Safety index, ratio of arrhythmogenic concentration to minimum positive inotropic effective concentration causing myocardial contraction in guinea pig left atrial muscles2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Cardiac glycosides from Antiaris toxicaria with potent cardiotonic activity.
AID127352Binding affinity against human monoclonal antibody (mAb)-7F22002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Three-dimensional quantitative structure-activity relationship analysis of ligand binding to human sequence antidigoxin monoclonal antibodies using comparative molecular field analysis.
AID77698Inotropic activity on electrically driven isolated Guinea pig atria2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Inotropic activity of hydroindene amidinohydrazones.
AID1072831Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Cytotoxic cardiac glycosides and coumarins from Antiaris toxicaria.
AID1455007Inhibition of recombinant rat Na+/K+-ATPase alpha4/beta1 expressed in baculovirus infected insect Sf9 cell membranes using [gamma-32P]ATP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins in presence of Na+, K+ an2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Design, Synthesis, and in Vitro and in Vivo Evaluation of Ouabain Analogues as Potent and Selective Na,K-ATPase α4 Isoform Inhibitors for Male Contraception.
AID1072825Cytotoxicity against human SK-MEL-2 cells assessed as growth inhibition after 72 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
Cytotoxic cardiac glycosides and coumarins from Antiaris toxicaria.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (550)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990375 (68.18)18.7374
1990's108 (19.64)18.2507
2000's44 (8.00)29.6817
2010's20 (3.64)24.3611
2020's3 (0.55)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.92

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 Index25.92 (24.57)
Research Supply Index6.35 (2.92)
Research Growth Index4.09 (4.65)
Search Engine Demand Index54.32 (26.88)
Search Engine Supply Index3.48 (0.95)

This Compound (25.92)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (0.88%)5.53%
Reviews10 (1.76%)6.00%
Case Studies3 (0.53%)4.05%
Observational0 (0.00%)0.25%
Other549 (96.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]