Page last updated: 2024-12-06

metrifudil

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

Cross-References

ID SourceID
PubMed CID65710
CHEMBL ID331382
SCHEMBL ID472516
MeSH IDM0220682

Synonyms (29)

Synonym
gtpl426
metrifudil
bdbm50080390
(2r,3s,4r,5r)-2-hydroxymethyl-5-[6-(2-methyl-benzylamino)-purin-9-yl]-tetrahydro-furan-3,4-diol
(2r,3r,4s,5r)-2-(6-(2-methyl-benzylamino)-9h-purin-9-yl)-5-(hydroxymethyl)-tetrahydrofuran-3,4-diol
(2r,3s,4r,5r)-2-(hydroxymethyl)-5-[6-[(2-methylphenyl)methylamino]purin-9-yl]oxolane-3,4-diol
CHEMBL331382 ,
th 322
th-322
metrifudil [inn]
unii-7k4gkq4xse
7k4gkq4xse ,
6-(o-methylbenzylamino)-9-beta-d-ribofuranosyl-9h-purine
23707-33-7
y 341
metrifudilum [inn-latin]
y-341
metrifudilum
tox21_110187
cas-23707-33-7
dtxcid9025168
dtxsid1045168 ,
n-[(2-methylphenyl)methyl]adenosine
6-(o-methylbenzylamino)-9-.beta.-d-ribofuranosyl-9h-purine
n6 -(2-methylbenzyl)adenosine
SCHEMBL472516
OOEMZCZWZXHBKW-SCFUHWHPSA-N
Q27085930
AKOS040753044

Research Excerpts

Bioavailability

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

Dosage Studied

ExcerptRelevanceReference
" Neuroprotective properties assessed after postischemic dosing in a Mongolian gerbil severe temporary forebrain ischemia paradigm, using hippocampal CA1 damage endpoints, and the efficacy of these agonists in an A(1) functional assay show similarities to some reference adenosine agonists."( N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
Hansen, AJ; Judge, ME; Knutsen, LJ; Lau, J; Petersen, H; Shalmi, M; Sheardown, MJ; Thomsen, C; Weis, JU, 1999
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency19.24710.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency26.83250.000221.22318,912.5098AID743035; AID743063
estrogen nuclear receptor alphaHomo sapiens (human)Potency2.19360.000229.305416,493.5996AID743069; AID743075
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency26.83250.001019.414170.9645AID743094
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency13.33320.001723.839378.1014AID743083
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency1.05910.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency1.05910.011912.222168.7989AID651632
[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)
Glyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)IC50 (µMol)700.00006.00007.33338.0000AID75595
Adenosine receptor A3Homo sapiens (human)Ki0.22440.00000.930610.0000AID1799500; AID239092
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.09800.00011.20929.9700AID32482
Adenosine receptor A3Rattus norvegicus (Norway rat)Ki0.19900.00030.91969.0000AID239053; AID33337
Adenosine receptor A2aHomo sapiens (human)Ki0.40260.00001.06099.7920AID1799500; AID239113
Adenosine receptor A2bHomo sapiens (human)Ki0.28350.00021.635210.0000AID1799500
Adenosine receptor A1Homo sapiens (human)Ki0.22240.00020.931610.0000AID1799500; AID239011
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (140)

Processvia Protein(s)Taxonomy
microtubule cytoskeleton organizationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
positive regulation of cytokine productionGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
glucose metabolic processGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
glycolytic processGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
negative regulation of endopeptidase activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
regulation of macroautophagyGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
negative regulation of translationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
killing of cells of another organismGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
positive regulation of type I interferon productionGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
peptidyl-cysteine S-trans-nitrosylationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
protein stabilizationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
defense response to fungusGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
neuron apoptotic processGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
killing by host of symbiont cellsGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptideGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cellular response to type II interferonGlyceraldehyde-3-phosphate dehydrogenaseHomo 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)
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)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo 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 (30)

Processvia Protein(s)Taxonomy
glyceraldehyde-3-phosphate dehydrogenase (NAD+) (phosphorylating) activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
protein bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
microtubule bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
aspartic-type endopeptidase inhibitor activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
peptidyl-cysteine S-nitrosylase activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
identical protein bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
NADP bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
NAD bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
disordered domain specific bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo 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)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
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 (34)

Processvia Protein(s)Taxonomy
nucleusGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cytoplasmGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
lipid dropletGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cytosolGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
plasma membraneGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
microtubule cytoskeletonGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
membraneGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
nuclear membraneGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
vesicleGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
intracellular membrane-bounded organelleGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
perinuclear region of cytoplasmGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
extracellular exosomeGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
GAIT complexGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
ribonucleoprotein complexGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cytosolGlyceraldehyde-3-phosphate dehydrogenaseHomo 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 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)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
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 (43)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID288179Antitumor activity against human CEM cells after 72 hrs by Calcein AM assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
AID288180Antitumor activity against human HL60 cells after 72 hrs by Calcein AM assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
AID239053Inhibition of [125I]AB-MECA binding to rat Adenosine A3 receptor expressed in CHO cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
AID251591Relative activation of human Adenosine A2B receptor after 10 uM treatment compared to 10 uM Cl-IB-MECA; Not determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
AID75230Reduction in hippocampal cell death by compound administered 30 min after a period of severe forebrain ischemia in the Mongolian gerbil at 0.3 mg/kg dosed 30 min and 120 min post ischemia1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID33792Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors.
AID239011Inhibition of [3H]R-PIA binding to human Adenosine A1 receptor expressed in CHO cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
AID239113Inhibition of [3H]-CGS- 21680 binding to human Adenosine A2A receptor expressed in CHO cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
AID33337Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors.
AID155528evaluated for the inhibition of Trypanosoma brucei Phosphoglycerate kinase (PGK); inactive at 4 mM2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Adenosine analogues as inhibitors of Trypanosoma brucei phosphoglycerate kinase: elucidation of a novel binding mode for a 2-amino-N(6)-substituted adenosine.
AID288181Antitumor activity against human G361 cells after 72 hrs by Calcein AM assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
AID30499Acidic dissociation constant(pKa) against A2 adenosine receptor of coronary artery1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Dog coronary artery adenosine receptor: structure of the N6-aryl subregion.
AID288169Cytokinin activity in wheat assessed as retention of chlorophyll in excised wheat leaves at 0.1 mmol/L relative to 6-Benzylaminopurine by senescence assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
AID184461Mean blood pressure(MBP) at an infused dose of agonist administered intravenously 0 mg/kg/h1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID288177Antitumor activity against human K562 cells after 72 hrs by Calcein AM assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
AID239092Inhibition of [125I]-AB-MECA binding to human Adenosine A3 receptor expressed in CHO cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
AID195500Percent reduction in blood pressure, in an anesthetized rat (administered 0.1 mg/kg intravenously bolus for 5 min)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID25506Index of hydrophobicity (k')1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Dog coronary artery adenosine receptor: structure of the N6-aryl subregion.
AID184462Mean blood pressure(MBP) at an infused dose of agonist administered intravenously 0.004 mg/kg/h1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID288183Cytotoxicity against mouse NIH 3T3 cells after 72 hrs by Calcein AM assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
AID288178Antitumor activity against human MCF cells after 72 hrs by Calcein AM assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
AID30496Molar potency ratio (MPR) against adenosine A2 receptor of canine coronary artery1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Dog coronary artery adenosine receptor: structure of the N6-aryl subregion.
AID32482Displacement of [3H]R-PIA from adenosine A1 receptor of Wistar rat forebrain1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID31885Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors.
AID184470Percent reduction in blood pressure in an anesthetized rat 5 min after intravenous administration of 0.1 mg/kg of compound1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID184464Mean blood pressure(MBP) at an infused dose of agonist administered intravenously 0.08 mg/kg/h1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID251590Relative activation of human Adenosine A3 receptor expressed in CHO cells at 10 uM treatment compared to 10 uM Cl-IB-MECA2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
AID130698In vivo inhibition of DMCM-induced seizures in mouse by the compound 30 min after intraperitoneal administration1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID30350Displacement of [3H]-CGS- 21680 from adenosine A2A receptor of rat striatal tissue1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID130702In vivo inhibition of spontaneous locomotor activity of mouse by the compound 30 min after intraperitoneal administration.1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID288176Antitumor activity against human HOS cells after 72 hrs by Calcein AM assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
AID288173Cytokinin activity in tobacco assessed as stimulation of callus growth at at 1 umol/L relative to 6-Benzylaminopurine2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
AID75595Inhibitory activity measured for Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) in Leishmania. mexicana1998Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24
Selective tight binding inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase via structure-based drug design.
AID73904Negative inotropy effect in isolated guinea pig atria. 1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID288182Antitumor activity against mouse B16 cells after 72 hrs by Calcein AM assay2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
AID53750In vitro inhibition of isoprenaline-stimulated cAMP accumulation in DDT1-MF2 cells (measured by adenosine A1 functional assay)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
AID288167Cytokinin activity in Amaranthus cotyledons assessed as dark induction of betacyanin synthesis at 0.1 mmol/L relative to 6-Benzylaminopurine2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Preparation, biological activity and endogenous occurrence of N6-benzyladenosines.
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.
AID1799500Binding Assay from Article 10.1016/j.chembiol.2004.12.010: \\A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.\\2005Chemistry & biology, Feb, Volume: 12, Issue:2
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (6.25)18.7374
1990's7 (43.75)18.2507
2000's6 (37.50)29.6817
2010's1 (6.25)24.3611
2020's1 (6.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]