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psb603

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Description

PSB603: an adenosine A2B receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44185871
CHEMBL ID483688
SCHEMBL ID17387706
SCHEMBL ID20883015
MeSH IDM000598884

Synonyms (26)

Synonym
8-(4-(4-(4-chlorophenyl)piperazine-1-sulfonyl)phenyl)-1-propyl-3,7-dihydropurine-2,6-dione
bdbm50268232
CHEMBL483688 ,
psb 603
gtpl5728
[3h]psb603
gtpl3284
psb-603
psb603
8-{4-[4-(4-chlorophenyl)piperazine-1-sulfonyl]phenyl}-1-propyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione
1092351-10-4
AKOS024457472
SCHEMBL17387706
J-002249
(8-[4-[4-(4-chlorophenyl)piperazine-1-sulfonyl)phenyl]]-1-propylxanthine
psb-603, >=98% (hplc)
Q27088474
8-(4-((4-(4-chlorophenyl)piperazin-1-yl)sulfonyl)phenyl)-2-hydroxy-1-propyl-1h-purin-6(7h)-one
SCHEMBL20883015
MS-29794
HY-103166
8-[4-[4-(4-chlorophenyl)piperazin-1-yl]sulfonylphenyl]-1-propyl-3,7-dihydropurine-2,6-dione
EN300-342765
8-(4-{[4-(4-chlorophenyl)piperazin-1-yl]sulfonyl}phenyl)-1-propyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione
CS-0025041
Z2217007926
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine receptor A3Homo sapiens (human)Ki10.00000.00000.930610.0000AID1375297; AID372152
Adenosine receptor A1Rattus norvegicus (Norway rat)IC50 (µMol)0.00050.00020.552110.0000AID1375317
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki10.00000.00011.20929.9700AID372147
Adenosine receptor A3Rattus norvegicus (Norway rat)IC50 (µMol)0.00070.00070.03740.0957AID1375318
Adenosine receptor A2aHomo sapiens (human)Ki5.00030.00001.06099.7920AID1871328; AID372150
Adenosine receptor A2bHomo sapiens (human)IC50 (µMol)0.00520.00050.30231.5000AID1375312; AID1375317; AID1375318; AID372163
Adenosine receptor A2bHomo sapiens (human)Ki0.00090.00021.635210.0000AID1814733; AID372151
Adenosine receptor A1Homo sapiens (human)Ki10.00000.00020.931610.0000AID372148
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki10.00000.00021.494010.0000AID372149
[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)
Adenosine receptor A2bHomo sapiens (human)Kd0.00050.00040.51913.0700AID372164; AID372168
Adenosine receptor A2bMus musculus (house mouse)Kd0.00040.00040.00040.0004AID372176
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (105)

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)
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)
temperature homeostasisAdenosine receptor A1Homo sapiens (human)
response to hypoxiaAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of respiratory gaseous exchange by nervous system processAdenosine receptor A1Homo sapiens (human)
negative regulation of acute inflammatory responseAdenosine receptor A1Homo sapiens (human)
negative regulation of leukocyte migrationAdenosine receptor A1Homo sapiens (human)
positive regulation of peptide secretionAdenosine receptor A1Homo sapiens (human)
positive regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
negative regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
regulation of glomerular filtrationAdenosine receptor A1Homo sapiens (human)
protein targeting to membraneAdenosine receptor A1Homo sapiens (human)
phagocytosisAdenosine receptor A1Homo sapiens (human)
inflammatory responseAdenosine receptor A1Homo sapiens (human)
signal transductionAdenosine receptor A1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
cell-cell signalingAdenosine receptor A1Homo sapiens (human)
nervous system developmentAdenosine receptor A1Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A1Homo sapiens (human)
response to inorganic substanceAdenosine receptor A1Homo sapiens (human)
negative regulation of glutamate secretionAdenosine receptor A1Homo sapiens (human)
response to purine-containing compoundAdenosine receptor A1Homo sapiens (human)
lipid catabolic processAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicAdenosine receptor A1Homo sapiens (human)
positive regulation of nucleoside transportAdenosine receptor A1Homo sapiens (human)
negative regulation of neurotrophin productionAdenosine receptor A1Homo sapiens (human)
positive regulation of protein dephosphorylationAdenosine receptor A1Homo sapiens (human)
vasodilationAdenosine receptor A1Homo sapiens (human)
negative regulation of circadian sleep/wake cycle, non-REM sleepAdenosine receptor A1Homo sapiens (human)
negative regulation of apoptotic processAdenosine receptor A1Homo sapiens (human)
positive regulation of potassium ion transportAdenosine receptor A1Homo sapiens (human)
positive regulation of MAPK cascadeAdenosine receptor A1Homo sapiens (human)
negative regulation of hormone secretionAdenosine receptor A1Homo sapiens (human)
cognitionAdenosine receptor A1Homo sapiens (human)
leukocyte migrationAdenosine receptor A1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
positive regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
regulation of sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergicAdenosine receptor A1Homo sapiens (human)
fatty acid homeostasisAdenosine receptor A1Homo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A1Homo sapiens (human)
long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
mucus secretionAdenosine receptor A1Homo sapiens (human)
negative regulation of mucus secretionAdenosine receptor A1Homo sapiens (human)
triglyceride homeostasisAdenosine receptor A1Homo sapiens (human)
regulation of cardiac muscle cell contractionAdenosine receptor A1Homo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic potentiationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

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 receptor bindingAdenosine receptor A1Homo sapiens (human)
purine nucleoside bindingAdenosine receptor A1Homo sapiens (human)
protein bindingAdenosine receptor A1Homo sapiens (human)
heat shock protein bindingAdenosine receptor A1Homo sapiens (human)
G-protein beta/gamma-subunit complex bindingAdenosine receptor A1Homo sapiens (human)
heterotrimeric G-protein bindingAdenosine receptor A1Homo sapiens (human)
protein heterodimerization activityAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A1Homo 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 (19)

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)
plasma membraneAdenosine receptor A1Homo sapiens (human)
plasma membraneAdenosine receptor A1Homo sapiens (human)
basolateral plasma membraneAdenosine receptor A1Homo sapiens (human)
axolemmaAdenosine receptor A1Homo sapiens (human)
asymmetric synapseAdenosine receptor A1Homo sapiens (human)
presynaptic membraneAdenosine receptor A1Homo sapiens (human)
neuronal cell bodyAdenosine receptor A1Homo sapiens (human)
terminal boutonAdenosine receptor A1Homo sapiens (human)
dendritic spineAdenosine receptor A1Homo sapiens (human)
calyx of HeldAdenosine receptor A1Homo sapiens (human)
postsynaptic membraneAdenosine receptor A1Homo sapiens (human)
presynaptic active zoneAdenosine receptor A1Homo sapiens (human)
synapseAdenosine receptor A1Homo sapiens (human)
dendriteAdenosine receptor A1Homo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (46)

Assay IDTitleYearJournalArticle
AID372158Displacement of [3H]MSX-2 from rat brain striatum adenosine A2A receptor at 10 uM2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372163Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-22009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1370514Cytotoxicity against human A549 cells assessed as cell viability at 0.1 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID1370515Cytotoxicity against human A549 cells assessed as cell viability at 1 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID372167Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells assessed as dissociation half life at 0.3 nM after 95 mins in presence of DPCPX by kinetic experiment2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372149Displacement of [3H]MSX-2 from rat brain striatum adenosine A2A receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1744277Antimigratory activity in human LNCaP cells assessed as reduction in cell migration at Ki level incubated for 72 hrs by crystal violet staining based confocal microscopy2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
3,4-Dihydropyrimidin-2(1
AID372154Displacement of [3H]CCPA from rat brain cortex adenosine A1 receptor at 10 uM2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1744278Antimetastatic activity in human PC-3 cells assessed as effect on cell shape at Ki level incubated for 72 hrs by confocal laser scanning microscopy2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
3,4-Dihydropyrimidin-2(1
AID1814733Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Development of Covalent, Clickable Probes for Adenosine A
AID1744279Antimetastatic activity in human PC-3 cells assessed as induction of actin skeleton reorganization at Ki level incubated for 72 hrs by confocal laser scanning microscopy2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
3,4-Dihydropyrimidin-2(1
AID1375317Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Fluorescent-Labeled Selective Adenosine A
AID372136Selectivity ratio of Ki for human recombinant adenosine A1 receptor to Ki for rat brain cortex adenosine A1 receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1370516Cytotoxicity against human A549 cells assessed as cell viability at 10 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID372147Displacement of [3H]CCPA from rat brain cortex adenosine A1 receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372156Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells at 10 uM2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1744275Antimigratory activity in human PC-3 cells assessed as reduction in cell migration at Ki level incubated for 72 hrs by crystal violet staining based confocal microscopy2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
3,4-Dihydropyrimidin-2(1
AID1370513Antiviral activity against Zika virus infected in human A549 cells preincubated for 5 hrs followed by compound wash measured after 48 hrs by viral plague-forming assay2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID1375297Displacement of [3H]PSB-11 from recombinant human adenosine A3 receptor expressed in CHO cell membranes after 180 mins by liquid scintillation counting method2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Fluorescent-Labeled Selective Adenosine A
AID1549341Semi-thermodynamic solubility of the compound at 200 uM after 24 hrs by LC/MS-based shake-flask method2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
A
AID372164Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372166Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells assessed as association half life at 0.3 nM after 180 mins by kinetic experiment2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1370517Cytotoxicity against human A549 cells assessed as cell viability at 100 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID372168Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1744276Antimigratory activity in human DU-145 cells assessed as reduction in cell migration at Ki level incubated for 72 hrs by crystal violet staining based confocal microscopy2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
3,4-Dihydropyrimidin-2(1
AID372151Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372148Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372159Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells at 10 uM2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372162Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells at 10 uM2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372176Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1375318Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Fluorescent-Labeled Selective Adenosine A
AID372177Selectivity ratio of Ki for human recombinant adenosine A2A receptor to Ki for rat brain striatum adenosine A2A receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372165Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells assessed as specific binding at 0.3 nM by kinetic experiment2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372178Activity at mouse recombinant adenosine A2B receptor expressed in CHO cells assessed per mg of protein2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372152Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1871328Antagonist activity at adenosine A2A receptor (unknown origin)2022European journal of medicinal chemistry, Jan-05, Volume: 227Adenosine receptor antagonists: Recent advances and therapeutic perspective.
AID372150Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1375312Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bov2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Fluorescent-Labeled Selective Adenosine A
AID372169Activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed per mg of protein by saturation experiment2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1345735Mouse A2B receptor (Adenosine receptors)2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1345822Human A3 receptor (Adenosine receptors)2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1345721Human A2B receptor (Adenosine receptors)2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1345690Rat A2A receptor (Adenosine receptors)2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1345685Human A1 receptor (Adenosine receptors)2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1345630Rat A1 receptor (Adenosine receptors)2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID1345618Human A2A receptor (Adenosine receptors)2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (7.14)29.6817
2010's9 (64.29)24.3611
2020's4 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.91

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 Index22.91 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index5.73 (4.65)
Search Engine Demand Index19.78 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.91)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (7.14%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (92.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]