Page last updated: 2024-11-08

sch 58261

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

Cross-References

ID SourceID
PubMed CID176408
CHEMBL ID17127
CHEBI ID93424
SCHEMBL ID537287
MeSH IDM0259122

Synonyms (64)

Synonym
160098-96-4
2-furan-2-yl-7-phenethyl-7h-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-ylamine(sch 58261)
bdbm50048466
2-furan-2-yl-7-phenethyl-7h-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-ylamine
2-(furan-2-yl)-7-phenethyl-7h-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine
HMS3268F20
BRD-K81225797-001-01-5
[3h]sch 58261
gtpl403
gtpl431
4-(furan-2-yl)-10-(2-phenylethyl)-3,5,6,8,10,11-hexaazatricyclo[7.3.0.0^{2,6}]dodeca-1(9),2,4,7,11-pentaen-7-amine
PDSP2_001183
PDSP1_001199
sch58261
NCGC00092350-01
7h-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidin-5-amine, 2-(2-furanyl)-7-(2-phenylethyl)-
sch 58261
sch-58261
5-amino-7-(2-phenylethyl)-2-(2-furyl)-pyrazolo(4,3-e)-1,2,4-triazolo(1,5-c)pyrimidine
NCGC00092350-02
sp-341
L000548
CHEMBL17127 ,
unii-4309023mah
4309023mah ,
HMS3263L20
FT-0643554
7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine
LP01259
S8104
CCG-222563
AKOS022181216
UTLPKQYUXOEJIL-UHFFFAOYSA-N ,
5-amino-7-(phenylethyl)-2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine
[3h]-sch 58261
SCHEMBL537287
NCGC00261944-01
tox21_501259
2-(2-furanyl)-7-(2-phenylethyl)-7h-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine
c18h15n7o
AC-32732
DTXSID80166799
mfcd00933778
HY-19533
CS-5639
CHEBI:93424
sch 58261, >=98% (hplc), solid
J-009674
EX-A1464
HMS3677A10
AS-16830
BCP14638
HMS3413A10
Q7389140
4-(furan-2-yl)-10-(2-phenylethyl)-3,5,6,8,10,11-hexazatricyclo[7.3.0.0^{2,6]dodeca-1(9),2,4,7,11-pentaen-7-amine
4-(furan-2-yl)-10-(2-phenylethyl)-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-7-amine
SDCCGSBI-0633817.P001
7h-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, 2-(2-furanyl)-7-(2-phenylethyl)-
HMS3886N04
NCGC00092350-09
AMY31049
HMS3748I07
BS162679
C3599

Research Excerpts

Overview

SCH 58261 is a reported adenosine A(2A) receptor antagonist. It is active in rat in vivo models of Parkinson's Disease upon ip administration.

ExcerptReferenceRelevance
"SCH 58261 is a reported adenosine A(2A) receptor antagonist which is active in rat in vivo models of Parkinson's Disease upon ip administration. "( Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists.
Boyle, CD; Chackalamannil, S; Cohen-Williams, ME; Greenlee, WJ; Higgins, GA; Lachowicz, JE; Lankin, CM; Neustadt, BR; Ng, K; Shah, U; Varty, GB; Zhang, H, 2008
)
2.02
"SCH 58261 is a reported adenosine A(2A) receptor antagonist, which is active in rat in vivo models of Parkinson's Disease upon ip administration. "( Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists.
Arik, L; Boyle, CD; Chackalamannil, S; Foster, C; Greenlee, WJ; Lachowicz, JE; Lindo, N; Monopoli, A; Neustadt, BR; Ng, K; Shah, U; Wang, S; Zhai, Y, 2008
)
2.06

Bioavailability

ExcerptReferenceRelevance
" Many compounds within this piperazine series of [1,2,4]triazolo[1,5-a]triazine have now been shown to have good oral bioavailability in the rat, with some as high as 89% (compound 35)."( Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
Chen, L; Engber, T; Grant, D; Hetu, G; Huang, C; Jin, X; Kumaravel, G; Peng, B; Petter, RC; Phadke, D; Reilly, J; Smits, G; Tam, S; Vu, CB; Zhang, J, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
triazolopyrimidines
[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]

Pathways (1)

PathwayProteinsCompounds
Purinergic signaling053

Protein Targets (54)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency25.11890.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency25.11890.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency11.22020.177814.390939.8107AID2147
Nrf2Homo sapiens (human)Potency0.73080.09208.222223.1093AID624149
thioredoxin reductaseRattus norvegicus (Norway rat)Potency5.71520.100020.879379.4328AID588453; AID588456
15-lipoxygenase, partialHomo sapiens (human)Potency19.95260.012610.691788.5700AID887
ATAD5 protein, partialHomo sapiens (human)Potency10.31830.004110.890331.5287AID493106
GLS proteinHomo sapiens (human)Potency11.22020.35487.935539.8107AID624146
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency14.12540.011212.4002100.0000AID1030
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency10.59090.001530.607315,848.9004AID1224821
ParkinHomo sapiens (human)Potency4.61090.819914.830644.6684AID720573
arylsulfatase AHomo sapiens (human)Potency5.35821.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency17.78280.035520.977089.1251AID504332
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency5.80480.01262.451825.0177AID485313
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency20.81140.316212.443531.6228AID902; AID924
D(1A) dopamine receptorHomo sapiens (human)Potency2.05950.02245.944922.3872AID488982
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency17.78280.001815.663839.8107AID894
chromobox protein homolog 1Homo sapiens (human)Potency5.62340.006026.168889.1251AID488953
mitogen-activated protein kinase 1Homo sapiens (human)Potency6.30960.039816.784239.8107AID1454
ras-related protein Rab-9AHomo sapiens (human)Potency8.91250.00022.621531.4954AID485297
survival motor neuron protein isoform dHomo sapiens (human)Potency2.23870.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency31.62280.031610.279239.8107AID884; AID885
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Integrin beta-3Homo sapiens (human)Potency31.62280.316211.415731.6228AID924
Integrin alpha-IIbHomo sapiens (human)Potency31.62280.316211.415731.6228AID924
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency28.18381.000010.475628.1838AID1457
GABA theta subunitRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Ataxin-2Homo sapiens (human)Potency1.58490.011912.222168.7989AID588378
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency1.69440.060110.745337.9330AID485368
[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)
CholinesteraseHomo sapiens (human)Ki5.00050.00001.51739.7300AID436525; AID436526
Adenosine receptor A3Homo sapiens (human)Ki7.45710.00000.930610.0000AID1138025; AID1810012; AID33046; AID34881; AID34890; AID436526; AID637479
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.12100.00011.20929.9700AID32340; AID32516
Adenosine receptor A1Bos taurus (cattle)Ki0.35700.00000.71316.0000AID31983
Adenosine receptor A2aHomo sapiens (human)IC50 (µMol)0.02600.00071.559410.0000AID1748871; AID93148
Adenosine receptor A2aHomo sapiens (human)Ki0.00160.00001.06099.7920AID1138023; AID1696175; AID1810053; AID1873115; AID239503; AID254299; AID34235; AID343333; AID343727; AID34373; AID34843; AID365580; AID436525; AID476441; AID637451; AID763042; AID763043
Adenosine receptor A2bHomo sapiens (human)IC50 (µMol)2.00000.00050.30231.5000AID1748872
Adenosine receptor A2bHomo sapiens (human)Ki4.49510.00021.635210.0000AID1138021; AID1696176; AID1810014; AID33296; AID637491
Adenosine receptor A2bRattus norvegicus (Norway rat)Ki1.00000.00061.353610.0000AID33611
Adenosine receptor A1Homo sapiens (human)Ki0.41370.00020.931610.0000AID1138024; AID1810015; AID1873116; AID30442; AID30443; AID30473; AID31077; AID476442; AID637450
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki0.23240.00021.494010.0000AID239020; AID239096; AID239133; AID239189; AID239479; AID32887; AID33015; AID33931; AID33934
Delta-type opioid receptorMus musculus (house mouse)Ki0.00060.00000.53939.4000AID365580
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.00060.00000.27869.0000AID365580
[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 A2aHomo sapiens (human)Kd0.00650.00020.47319.6000AID1342781; AID1342783; AID1342793; AID1342797; AID1342798
[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 A2aHomo sapiens (human)ED500.30000.30000.30000.3000AID224014
Adenosine receptor A2aHomo sapiens (human)K0.00100.00100.00170.0023AID1871401
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (191)

Processvia Protein(s)Taxonomy
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
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)
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)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (43)

Processvia Protein(s)Taxonomy
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
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)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (56)

Processvia Protein(s)Taxonomy
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
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 membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
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)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (119)

Assay IDTitleYearJournalArticle
AID1345822Human A3 receptor (Adenosine receptors)2006Nature reviews. Drug discovery, Mar, Volume: 5, Issue:3
Adenosine receptors as therapeutic targets.
AID1345721Human A2B receptor (Adenosine receptors)2000Molecular pharmacology, Dec, Volume: 58, Issue:6
Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine.
AID1345685Human A1 receptor (Adenosine receptors)1999Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 359, Issue:1
Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.
AID1345618Human A2A receptor (Adenosine receptors)1999Biochemical pharmacology, Jan-01, Volume: 57, Issue:1
Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
AID1345685Human A1 receptor (Adenosine receptors)2006Nature reviews. Drug discovery, Mar, Volume: 5, Issue:3
Adenosine receptors as therapeutic targets.
AID1345685Human A1 receptor (Adenosine receptors)1994The Journal of biological chemistry, Jan-28, Volume: 269, Issue:4
A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding.
AID1345618Human A2A receptor (Adenosine receptors)1997British journal of pharmacology, Jun, Volume: 121, Issue:3
Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
AID1345721Human A2B receptor (Adenosine receptors)2006Nature reviews. Drug discovery, Mar, Volume: 5, Issue:3
Adenosine receptors as therapeutic targets.
AID1345618Human A2A receptor (Adenosine receptors)1999Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 359, Issue:1
Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.
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.
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
AID1810051Inhibition of HDAC1 (unknown origin) assessed as release of 7-amino-4-methylcoumarin incubated in room temperature for 15 min measured by Spectra max microtitre plate reader
AID1810015Displacement of [3H]DPCPX from human adenosine A1 receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis
AID1871401Binding affinity to human adenosine A2A receptor assessed as apparent first-order rate constant(kobs)2022European journal of medicinal chemistry, Jan-05, Volume: 227Adenosine receptor antagonists: Recent advances and therapeutic perspective.
AID476441Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by rapid filtration assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists.
AID281575Displacement of [3h]DPCPX from adenosine A receptor in rat cerebral cortex membrane2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists.
AID33611Displacement of [3H]-CGS- 21680 from rat striatal membrane adenosine A2B receptor2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.
AID34890Displacement of specific [3H]MRE3008-F20 binding at human adenosine A3 receptor expressed in CHO cells.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
AID1873116Antagonist activity at adenosine A1 receptor (unknown origin)2022European journal of medicinal chemistry, Jul-05, Volume: 237Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.
AID1871385Effect of compound in haloperidol-induced catalepsy in Swiss albino male mouse assessed as catalepsy score after 120 mins2022European journal of medicinal chemistry, Jan-05, Volume: 227Adenosine receptor antagonists: Recent advances and therapeutic perspective.
AID30442Binding affinity against adenosine A1 receptor in human cortical membranes using [3H]CHA as radioligand2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
AID637450Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cells after 120 mins by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.
AID1810014Displacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis
AID343727Antagonist activity at human adenosine A2A receptor2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists.
AID33931Displacement [3H]-CGS-21,680 from Adenosine A2A receptor in rat striatal membrane.1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists.
AID1138024Inhibition of human recombinant adenosine A1 receptor2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Adenosine A2A receptor as a drug discovery target.
AID234767Selectivity for A1 and A2A adenosine receptors in rat1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
AID239479Binding affinity against Adenosine A2a receptor from rat brain tissue was determined using [3H]ZM-241385 as radioligand2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles.
AID32887Displacement of [3H]-CGS- 21680 from rat striatal membrane Adenosine A2A receptor2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.
AID33296Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
AID767603Inhibition of haloperidol-induced catalepsy in Swiss albino mouse at 10 mg/kg, ip administered 30 mins prior haloperidol challenge measured after 120 mins2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Design and synthesis of (4E)-4-(4-substitutedbenzylideneamino)-3-substituted-2,3-dihydro-2-thioxothiazole-5-carbonitrile as novel A2A receptor antagonists.
AID1138021Inhibition of human recombinant adenosine receptor A2b2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Adenosine A2A receptor as a drug discovery target.
AID239096Inhibition of [3H]ZM-241,385 binding to rat brain adenosine A2a receptor2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
AID239189Inhibition of [3H]ZM-241385 binding to adenosine A2a receptor of rat brain tissue2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
AID31077Displacement of [3H]CHA from human Adenosine A1 receptor expressed in CHO cells1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
AID32350Inhibition of [3H]-CHA binding to Adenosine A1 receptor in rat whole brain homogenates.1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists.
AID33059Selectivity ratio of human adenosine A3 receptor to human adenosine A2A receptor.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
AID763042Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Fluorescent ligands for adenosine receptors.
AID476444Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP accumulation at 100 nM after 24 hrs (Rvb= 0.40 pmol/ml)2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists.
AID343334Selectivity for human adenosine A2A receptor over human adenosine A1 receptor2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists.
AID32340Displacement of [3H]CHA from rat cortical membrane Adenosine A1 receptor2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.
AID343728Selectivity for human adenosine A2A receptor over human adenosine A1 receptor2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists.
AID33603Selectivity ratio of human adenosine A2B receptor to human adenosine A2A receptor.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
AID231273Ratio of binding affinity against bovine adenosine A1 to that of A2 receptor2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
AID1810049Antiproliferative activity against mouse CT26 cells measured after 72 hrs by CCK8 assay
AID239503Inhibition constant against human Adenosine A2a receptor using [3H]-SCH- 58261 as radioligand expressed in HEK cell membranes2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.
AID34235Binding affinity against human Adenosine A2a receptor (hA2a)2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?
AID1871353Effect of compound in haloperidol and NECA-induced catalepsy in mouse assessed as catalepsy score at 10 mg/kg measured after 120 mins2022European journal of medicinal chemistry, Jan-05, Volume: 227Adenosine receptor antagonists: Recent advances and therapeutic perspective.
AID239213Inhibition of [3H]DPCPX binding to rat cerebral cortex adenosine A1 receptor2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
AID224014Inhibition of the effects of NECA on ADP (5 uM)-induced rabbit platelet aggregation.1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists.
AID239464Binding affinity against Adenosine A1 receptor from rat cerebral cortex was determined using [3H]DPCPX as radioligand2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles.
AID235153Selectivity for A1 and A2A receptors1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists.
AID234927Selectivity for human A3 adenosine receptor and human A2A adenosine receptor1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
AID1696176Inhibition of human adenosine 2B receptor
AID1138025Inhibition of human recombinant adenosine A3 receptor2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Adenosine A2A receptor as a drug discovery target.
AID1138023Inhibition of human recombinant adenosine receptor A2a2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Adenosine A2A receptor as a drug discovery target.
AID1810012Displacement of [3H]DPCPX from human adenosine A3 receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis
AID234926Selectivity for human A1 adenosine receptor and human A2A adenosine receptor1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
AID343333Antagonist activity at human adenosine A2A receptor2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists.
AID1696175Antagonist activity at human adenosine 2A receptor
AID31085Selectivity ratio of human adenosine A1 receptor to human adenosine A2A receptor.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
AID32516Displacement of [3H]CHA from rat cortical membrane Adenosine A1 receptor. Parenthesis indicate 95% confidence limit.1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
AID30443Binding affinity against human Adenosine A1 receptor2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?
AID476443Selectivity ratio of Ki for human adenosine A1 receptor to Ki for human adenosine A2A receptor2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists.
AID763043Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS53462013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Fluorescent ligands for adenosine receptors.
AID244230Selectivity as the ratio of inhibition constants of human adenosine A1 receptor to that of human adenosine A2A receptor2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.
AID281574Displacement of [3H]ZM241385 from adenosine A2A receptor in rat brain membrane2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists.
AID34373Displacement of specific [3H]-SCH- 58261 binding at human Adenosine A2A receptor expressed in HEK293 cells.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
AID33934Inhibition of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal homogenates.1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists.
AID30795Binding affinity against adenosine A2 receptor in human striatal membranes using [3H]CGS-21680 as radioligand2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
AID239020Binding affinity towards Adenosine A2A receptor of rat brain tissues using [3H]ZM-241385 as radioligand2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists.
AID1873115Antagonist activity at adenosine A2A receptor (unknown origin)2022European journal of medicinal chemistry, Jul-05, Volume: 237Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.
AID31983Binding affinity against adenosine A1 receptor in bovine cortical membranes using [3H]CHA as radioligand2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
AID30473Displacement of specific [3H]DPCPX binding at human Adenosine A1 receptor expressed in CHO cells.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
AID767609Antagonist activity at human A2A receptor expressed in HEK293 cells assessed as decrease in NECA-induced cAMP release at 1 uM after 15 mins2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Design and synthesis of (4E)-4-(4-substitutedbenzylideneamino)-3-substituted-2,3-dihydro-2-thioxothiazole-5-carbonitrile as novel A2A receptor antagonists.
AID254299Binding affinity towards adenosine A2A receptor2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists.
AID239210Inhibition of [3H]DPCPX binding to adenosine A1 receptor of rat cerebral cortex2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
AID34881Displacement of [3H]-AB MECA from human Adenosine A3 receptor expressed in HEK293 cells2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.
AID1810050Antiproliferative activity against mouse MC38 cells measured after 72 hrs by CCK8 assay
AID239133Binding affinity against Adenosine A2a receptor determined using [3H]ZM-241385 as radioligand2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.
AID1810053Displacement of [3H]SCH58261 from adenosine A2A receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis
AID637479Displacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.
AID33046Displacement of [125I]AB-MECA from human Adenosine A3 receptor expressed in HEK293 cells1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
AID1138081Binding affinity to adenosine receptor A2a in rat striatum2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Adenosine A2A receptor as a drug discovery target.
AID1810052Inhibition of HDAC6 (unknown origin) assessed as release of 7-amino-4-methylcoumarin incubated in room temperature for 15 min measured by Spectra max microtitre plate reader
AID365580Binding affinity to human adenosine A2A receptor2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
AID476442Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in HEK293 cells after 60 mins by rapid filtration assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists.
AID637491Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.
AID767604Inhibition of haloperidol-induced catalepsy in Swiss albino mouse at 5 to 20 mg/kg, ip administered 30 mins prior haloperidol challenge measured after 120 mins2013Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
Design and synthesis of (4E)-4-(4-substitutedbenzylideneamino)-3-substituted-2,3-dihydro-2-thioxothiazole-5-carbonitrile as novel A2A receptor antagonists.
AID436525Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites.
AID637451Displacement of [3H]-ZM 241385 from human adenosine A2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.
AID93148Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
AID34843Displacement of [3H]-SCH- 58261 from human Adenosine A2A receptor expressed in CHO cells1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
AID234928Selectivity for human A3 adenosine receptor and rat A2A adenosine receptor1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
AID238943Binding affinity towards Adenosine A1 receptor of rat cerebral cortex using [3H]-DPCPX as radioligand2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists.
AID30487Binding affinity against adenosine A2 receptor in bovine striatal membranes using [3H]-CGS-21,680 as radioligand2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
AID239465Binding affinity against Adenosine A1 receptor from rat cerebral cortex was determined using [3H]DPCPX as radioligand2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.
AID33015Displacement of [3H]-CGS- 21680 from rat striatal membranes Adenosine A2A receptor. Parenthesis indicate 95% confidence limits.1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
AID231277Ratio of binding affinity against human adenosine A1 to that of A2 receptor2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
AID436526Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites.
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.
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).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (46)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's7 (15.22)18.2507
2000's19 (41.30)29.6817
2010's10 (21.74)24.3611
2020's10 (21.74)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.54

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

MetricThis Compound (vs All)
Research Demand Index25.54 (24.57)
Research Supply Index3.85 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.54)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews5 (10.87%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other41 (89.13%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]