Page last updated: 2024-12-04

8-(4-sulfophenyl)theophylline

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

8-(4-sulfophenyl)theophylline: adenosine antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1908
CHEMBL ID8488
SCHEMBL ID1320226
MeSH IDM0098763

Synonyms (51)

Synonym
EU-0100135
PDSP1_000449
lopac-a-013
NCGC00015000-01
PDSP2_000447
LOPAC0_000135
8-pspt
NCGC00093625-03
psp-theophylline
8-(p-sulfophenyl)theophylline
NCGC00093625-01
NCGC00093625-02
4-(1,3-dimethyl-2,6-dioxo-2,3,6,9-tetrahydro-1h-purin-8-yl)benzenesulfonic acid
STK505874
NCGC00015000-02
A-013
NCGC00015000-05
8-(p-sulfophenyl)thiophylline
CHEMBL8488 ,
4-(1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1h-purin-8-yl)benzenesulfonic acid
80206-91-3
8-sulphophenyltheophylline
benzenesulfonic acid, 4-(2,3,6,7-tetrahydro-1,3-dimethyl-2,6-dioxo-1h-purin-8-yl)-
8-(4-sulfophenyl)theophylline
4-(1,3-dimethyl-2,6-dioxo-7h-purin-8-yl)benzenesulfonic acid
4-(1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1h-purin-8-yl)-benzenesulfonic acid
nsc_1908
8-spt
bdbm82023
cas_80206-91-3
HMS3260K12
SCHEMBL1320226
CCG-204230
NCGC00015000-03
NCGC00015000-04
AKOS005172213
4-(2,3,6,7-tetrahydro-1,3-dimethyl-2,6-dioxo-1h-purin-8-yl)benzenesulfonic acid
LP00135
NCGC00260820-01
tox21_500135
DTXSID90230152
LXJSJIXZOAMHTG-UHFFFAOYSA-N
8-(p-sulfophenyl)-theophylline
8(p-sulfophenyl)theophylline
mfcd00545717
sr-01000075188
SR-01000075188-1
SDCCGSBI-0050123.P002
NCGC00015000-08
PD015424
benzenesulfonic acid, 4-(2,3,6,9-tetrahydro-1,3-dimethyl-2,6-dioxo-1h-purin-8-yl)-

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" This study was designed to characterise the dose-response relationship of adenosine on these variables relative to arrhythmia induction with single atrial premature stimuli."( Effects of adenosine on atrial refractoriness and arrhythmias.
Belardinelli, L; Buchanan, LV; Gibson, JK; Kabell, G, 1994
)
0.29
" The nitric oxide (NO) synthase inhibitor, L-monomethyl-L-arginine (30 microM) shifted the dose-response curve for NECA to the right in all groups suggesting that the vascular response to NECA is partially mediated through the release of NO."( Influence of aortic baroreceptor denervation on adenosine receptor-mediated relaxation of isolated rat aorta.
Abdel-Rahman, AA; el-Mas, MM; Fahim, M; Mustafa, SJ, 1994
)
0.29
" PPADS (3-100 microM) attenuated vasodilator responses to the P2Y-selective agonists 2MeSATP and ADP, shifting the dose-response curves to the right."( Discrimination by PPADS between endothelial P2Y- and P2U-purinoceptors in the rat isolated mesenteric arterial bed.
Burnstock, G; Ralevic, V, 1996
)
0.29
" Addition of P2Y1 blockade to P1 blockade shifted the ATP dose-response curve further rightward."( Nucleotide coronary vasodilation in guinea pig hearts.
Feigl, EO; Gorman, MW; Jacobson, KA; Ogimoto, K; Savage, MV, 2003
)
0.32
" Experiments with adenosine demonstrated that the selected dose of SPT elicited marked rightward shifts in the dose-response curves for both the inotropic and vascular actions."( Acute dilatory and negative inotropic effects of homocysteine are inhibited by an adenosine blocker.
Boerma, M; Hauer-Jensen, M; Joseph, J; Kennedy, RH; Melchert, RB; Owings, R, 2006
)
0.33
"Endogenous adenosine is an important modulator of intestinal neuro-effector activity, operating in the linear part of the dose-response curve."( Estimation of endogenous adenosine activity at adenosine receptors in guinea-pig ileum using a new pharmacological method.
Glaumann, C; Grishina, VA; Gustafsson, LE; Nilsson, KF, 2010
)
0.36
" Using a bivascular liver perfusion dose-response curves to adenosine of the HA were performed in the presence and the absence of pan-adenosine blocker (8-SPT), A1 blocker (caffeine) or nitric oxide synthase-blocker (l-NMMA) after preconstriction with an alpha1-agonist (methoxamine)."( A distinct nitric oxide and adenosine A1 receptor dependent hepatic artery vasodilatatory response in the CCl-cirrhotic liver.
Groszmann, RJ; Mehal, WZ; Ripoll, C; Zipprich, A, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency8.42440.025120.237639.8107AID886; AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency8.42440.025120.237639.8107AID886; AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency12.58930.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency35.48135.623417.292931.6228AID2323
Chain A, CruzipainTrypanosoma cruziPotency12.58930.002014.677939.8107AID1476
dopamine D1 receptorHomo sapiens (human)Potency4.61090.00521.30228.1995AID624455
thioredoxin reductaseRattus norvegicus (Norway rat)Potency21.49780.100020.879379.4328AID488772; AID488773; AID588453; AID588456
USP1 protein, partialHomo sapiens (human)Potency0.35480.031637.5844354.8130AID504865
NFKB1 protein, partialHomo sapiens (human)Potency0.14130.02827.055915.8489AID895; AID928
GLS proteinHomo sapiens (human)Potency0.10000.35487.935539.8107AID624146
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency25.11890.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency6.69520.531815.435837.6858AID504845
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency2.98490.001530.607315,848.9004AID1224821
glucocerebrosidaseHomo sapiens (human)Potency28.93420.01268.156944.6684AID2101
alpha-galactosidaseHomo sapiens (human)Potency34.89374.466818.391635.4813AID2107
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency39.81070.035520.977089.1251AID504332
cytochrome P450 2C19 precursorHomo sapiens (human)Potency31.62280.00255.840031.6228AID899
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency12.58930.001815.663839.8107AID894
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency39.81070.00419.962528.1838AID2675
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.08910.00106.000935.4813AID944
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency10.00001.000010.475628.1838AID1457
[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)
Adenosine receptor A3Homo sapiens (human)Ki8.44500.00000.930610.0000AID267468; AID33502
Adenosine receptor A1Rattus norvegicus (Norway rat)IC50 (µMol)0.44800.00020.552110.0000AID31393
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki2.12000.00011.20929.9700AID31856; AID31887; AID32177; AID32487; AID32491
Adenosine receptor A1Bos taurus (cattle)IC50 (µMol)0.02190.00001.09106.7400AID31836
Adenosine receptor A2aHomo sapiens (human)Ki5.25000.00001.06099.7920AID30797; AID33734
Adenosine receptor A2bHomo sapiens (human)Ki2.89800.00021.635210.0000AID267465; AID30797; AID33176; AID33180; AID33734
Adenosine receptor A2bRattus norvegicus (Norway rat)Ki5.25000.00061.353610.0000AID30797; AID33734
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki5.36000.00021.494010.0000AID30797; AID32862; AID33734
Adenosine receptor A2aCavia porcellus (domestic guinea pig)Ki6.30000.11002.63858.0000AID30621
[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)
Adenosine receptor A2bRattus norvegicus (Norway rat)Ratio1.50000.00330.82929.6000AID33746
Adenosine receptor A2aRattus norvegicus (Norway rat)Ratio1.50000.00330.82309.6000AID33746
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (66)

Processvia Protein(s)Taxonomy
inflammatory responseAdenosine receptor A3Homo sapiens (human)
signal transductionAdenosine receptor A3Homo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A3Homo sapiens (human)
regulation of heart contractionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A3Homo sapiens (human)
response to woundingAdenosine receptor A3Homo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell migrationAdenosine receptor A3Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityAdenosine receptor A3Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Bos taurus (cattle)
response to purine-containing compoundAdenosine receptor A1Bos taurus (cattle)
synaptic transmission, dopaminergicAdenosine receptor A2aHomo sapiens (human)
response to amphetamineAdenosine receptor A2aHomo sapiens (human)
regulation of DNA-templated transcriptionAdenosine receptor A2aHomo sapiens (human)
phagocytosisAdenosine receptor A2aHomo sapiens (human)
apoptotic processAdenosine receptor A2aHomo sapiens (human)
inflammatory responseAdenosine receptor A2aHomo sapiens (human)
cellular defense responseAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
cell-cell signalingAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, cholinergicAdenosine receptor A2aHomo sapiens (human)
central nervous system developmentAdenosine receptor A2aHomo sapiens (human)
blood coagulationAdenosine receptor A2aHomo sapiens (human)
sensory perceptionAdenosine receptor A2aHomo sapiens (human)
locomotory behaviorAdenosine receptor A2aHomo sapiens (human)
blood circulationAdenosine receptor A2aHomo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A2aHomo sapiens (human)
response to xenobiotic stimulusAdenosine receptor A2aHomo sapiens (human)
response to inorganic substanceAdenosine receptor A2aHomo sapiens (human)
positive regulation of glutamate secretionAdenosine receptor A2aHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionAdenosine receptor A2aHomo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A2aHomo sapiens (human)
response to purine-containing compoundAdenosine receptor A2aHomo sapiens (human)
response to caffeineAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
positive regulation of urine volumeAdenosine receptor A2aHomo sapiens (human)
vasodilationAdenosine receptor A2aHomo sapiens (human)
eating behaviorAdenosine receptor A2aHomo sapiens (human)
negative regulation of vascular permeabilityAdenosine receptor A2aHomo sapiens (human)
negative regulation of neuron apoptotic processAdenosine receptor A2aHomo sapiens (human)
positive regulation of circadian sleep/wake cycle, sleepAdenosine receptor A2aHomo sapiens (human)
negative regulation of alpha-beta T cell activationAdenosine receptor A2aHomo sapiens (human)
astrocyte activationAdenosine receptor A2aHomo sapiens (human)
neuron projection morphogenesisAdenosine receptor A2aHomo sapiens (human)
positive regulation of protein secretionAdenosine receptor A2aHomo sapiens (human)
negative regulation of inflammatory responseAdenosine receptor A2aHomo sapiens (human)
regulation of mitochondrial membrane potentialAdenosine receptor A2aHomo sapiens (human)
membrane depolarizationAdenosine receptor A2aHomo sapiens (human)
regulation of calcium ion transportAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
inhibitory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
prepulse inhibitionAdenosine receptor A2aHomo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2aHomo sapiens (human)
positive regulation of long-term synaptic potentiationAdenosine receptor A2aHomo sapiens (human)
positive regulation of apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
positive regulation of chronic inflammatory response to non-antigenic stimulusAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A2bHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionAdenosine receptor A2bHomo sapiens (human)
positive regulation of cGMP-mediated signalingAdenosine receptor A2bHomo sapiens (human)
cGMP-mediated signalingAdenosine receptor A2bHomo sapiens (human)
positive regulation of chemokine productionAdenosine receptor A2bHomo sapiens (human)
positive regulation of interleukin-6 productionAdenosine receptor A2bHomo sapiens (human)
mast cell degranulationAdenosine receptor A2bHomo sapiens (human)
positive regulation of mast cell degranulationAdenosine receptor A2bHomo sapiens (human)
relaxation of vascular associated smooth muscleAdenosine receptor A2bHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2bHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
vasodilationAdenosine receptor A2bHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
G protein-coupled adenosine receptor activityAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aHomo sapiens (human)
protein bindingAdenosine receptor A2aHomo sapiens (human)
calmodulin bindingAdenosine receptor A2aHomo sapiens (human)
lipid bindingAdenosine receptor A2aHomo sapiens (human)
enzyme bindingAdenosine receptor A2aHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingAdenosine receptor A2aHomo sapiens (human)
identical protein bindingAdenosine receptor A2aHomo sapiens (human)
protein-containing complex bindingAdenosine receptor A2aHomo sapiens (human)
alpha-actinin bindingAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2bHomo sapiens (human)
protein bindingAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor activityAdenosine receptor A2bHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
plasma membraneAdenosine receptor A3Homo sapiens (human)
presynaptic membraneAdenosine receptor A3Homo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A3Homo sapiens (human)
dendriteAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
synapseAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
intermediate filamentAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
membraneAdenosine receptor A2aHomo sapiens (human)
dendriteAdenosine receptor A2aHomo sapiens (human)
axolemmaAdenosine receptor A2aHomo sapiens (human)
asymmetric synapseAdenosine receptor A2aHomo sapiens (human)
presynaptic membraneAdenosine receptor A2aHomo sapiens (human)
neuronal cell bodyAdenosine receptor A2aHomo sapiens (human)
postsynaptic membraneAdenosine receptor A2aHomo sapiens (human)
presynaptic active zoneAdenosine receptor A2aHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2bHomo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A2bHomo sapiens (human)
presynapseAdenosine receptor A2bHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2bHomo sapiens (human)
plasma membraneAdenosine receptor A2bHomo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (66)

Assay IDTitleYearJournalArticle
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
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.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347151Optimization of GU AMC 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.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347169Tertiary RLuc qRT-PCR qHTS assay 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.
AID1347161Confirmatory 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.
AID1347149Furin counterscreen 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.
AID1347154Primary screen GU AMC 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.
AID1347152Confirmatory screen NINDS AMC 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.
AID1347167Vero cells viability 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.
AID1347168HepG2 cells viability 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.
AID1347153Confirmatory screen GU AMC 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.
AID32487Inhibition of 1 nM [3H]- N6 -(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat fat cell membrane1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
AID31390Binding affinity against adenosine A1 receptor in rat brain membrane preparations using N6-[3H]cyclohexyladenosine as a radioligand1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists.
AID267468Displacement of [125I]AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
AID229822Ratio of antagonism at A2 versus A1 receptors (Ki values)1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
AID30797Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via adenosine A2 receptor in human platelet membranes.1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID32491Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID32177Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID33734Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via Adenosine A2 receptor in rat PC12 membranes1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
AID21511Solubility in water1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
AID267463Displacement of [3H]MSX2 from human recombinant adenosine A2A receptor expressed in CHO cells2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
AID267460Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
AID33752Ratio of A2 to A1.1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID32046Binding affinity for adenosine A1 receptor using [3H]PIA in rat brain cortical membrane2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
AID205269Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID32862Binding affinity for adenosine A2A receptor from rat brain membranes using [3H]CGS-216801993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors.
AID30621Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
AID32636Binding affinity against adenosine A1 receptor in rat brain membrane preparations using N6-[3H]cyclohexyladenosine as radioligand, PCY = log (100000/IC50).1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists.
AID33176Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand2002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
AID31856Antagonism of binding of 1 nM [3H]cyclohexyladenosine to adenosine A1 receptors on rat cortical membranes1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID33502Binding affinity for human adenosine A3 receptor using [3H]-PBS-11 in CHO cell membranes2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
AID267459Displacement of [3H]R-PIA from adenosine A1 receptor in rat brain cortical membranes2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
AID32868Binding affinity for adenosine A2A receptor using [3H]-NECA in rat brain striatal membranes2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID33746Binding affinity against adenosine A2 receptor using [3H]- NECA as radioligand1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID267465Displacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cells2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
AID267462Displacement of [3H]R-PIA from adenosine A2A receptor in rat brain striatal membranes2006Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID31393Binding affinity against rat brain adenosine A1 receptor using N6-[3H]- cyclohexyladenosine1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.
AID31887Binding affinity for adenosine A1 receptor from rat brain membranes using [3H]PIA as radioligand1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors.
AID33180Binding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranes2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
AID31836Binding affinity against bovine brain adenosine A1 receptor by using N6-[3H]- cyclohexyladenosine1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
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 (319)

TimeframeStudies, This Drug (%)All Drugs %
pre-199029 (9.09)18.7374
1990's175 (54.86)18.2507
2000's78 (24.45)29.6817
2010's30 (9.40)24.3611
2020's7 (2.19)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.23

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index9.23 (24.57)
Research Supply Index5.79 (2.92)
Research Growth Index5.02 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.23)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.31%)5.53%
Reviews2 (0.62%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other321 (99.07%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]