v 2006 profile

3-(4-amino-3-methylbenzyl)-7-(2-furyl)-3H-(1,2,3)triazolo(4,5-d)pyrimidine-5-amine: antiparkinson agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	21874557
CHEMBL ID	447664
SCHEMBL ID	2849027
MeSH ID	M0543805

Synonym
bdbm50254013
3-(4-amino-3-methylbenzyl)-7-(2-furyl)-3h-[1,2,3]triazolo[4,5-d]pyrimidine-5-amine
ceb-4520
ver-11135
biib-014
ver-ado-49
ver-a00-11
ver-a00049
vr-2006
vipadenant
v-2006
CHEMBL447664 ,
ver-a-00049
v2006
biib014
ver-a-00-11
vipadenant (usan/inn)
442908-10-3
D09991
3-(4-amino-3-methylbenzyl)-7-(2-furyl)-3h-(1,2,3)triazolo(4,5-d)pyrimidine-5-amine
unii-ldr3ush1nj
v 2006
vipadenant [usan:inn]
ldr3ush1nj ,
biib 014
vipadenant [inn]
3-((4-amino-3-methylphenyl)methyl)-7-(furan-2-yl)-3h-(1,2,3)triazolo(4,5-d)pyrimidin-5-amine
1148126-34-4
vipadenant [usan]
vipadenant [who-dd]
3h-1,2,3-triazolo(4,5-d)pyrimidin-5-amine, 3-((4-amino-3-methylphenyl)methyl)-7-(2-furanyl)-
gtpl5612
3-[(4-amino-3-methylphenyl)methyl]-7-furan-2-yltriazolo[5,4-d]pyrimidin-5-amine
SCHEMBL2849027
HQSBCDPYXDGTCL-UHFFFAOYSA-N
3-(4-amino-3-methylbenzyl)-7-(furan-2-yl)-3h-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine
AC-35302
HY-10857
AKOS026750454
DTXSID90196103
EX-A1029
vipadenant; biib-014
3-[(4-amino-3-methylphenyl)methyl]-7-(2-furanyl)-3h-1,2,3-triazolo[4,5-d]pyrimidin-5-amine
9xt ,
3-[(4-azanyl-3-methyl-phenyl)methyl]-7-(furan-2-yl)-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine
BCP15984
DB06625
AS-35055
Q27089145
SB19840
mfcd12024697
biib-014; ceb-4520
biib014; ceb-4520
3-[(4-amino-3-methylphenyl)methyl]-7-(furan-2-yl)triazolo[4,5-d]pyrimidin-5-amine
A872563

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Adenosine receptor A3	Homo sapiens (human)	Ki	1.0050	0.0000	0.9306	10.0000	AID1138025; AID412506
Adenosine receptor A2a	Homo sapiens (human)	Ki	0.0012	0.0000	1.0609	9.7920	AID1138023; AID1871328; AID1907398; AID412503
Adenosine receptor A2b	Homo sapiens (human)	Ki	0.0630	0.0002	1.6352	10.0000	AID1138021; AID412505
Adenosine receptor A1	Homo sapiens (human)	Ki	0.0680	0.0002	0.9316	10.0000	AID1138024; AID412504
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Adenosine receptor A3	Homo sapiens (human)	Kd	1.5849	0.0001	0.4651	1.5849	AID412534
Adenosine receptor A2a	Homo sapiens (human)	Kd	0.0006	0.0002	0.4731	9.6000	AID412518
Adenosine receptor A2b	Homo sapiens (human)	Kd	0.0316	0.0004	0.5191	3.0700	AID412532
Adenosine receptor A1	Homo sapiens (human)	Kd	0.1000	0.0002	0.4621	5.9000	AID412533
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Adenosine receptor A3	Homo sapiens (human)	KA	1.5000	1.5000	1.5000	1.5000	AID412538
Adenosine receptor A2a	Homo sapiens (human)	KA	0.0006	0.0006	0.0006	0.0006	AID412535
Adenosine receptor A2b	Homo sapiens (human)	KA	0.0310	0.0310	0.0310	0.0310	AID412537
Adenosine receptor A1	Homo sapiens (human)	KA	0.0950	0.0950	0.0950	0.0950	AID412536
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
inflammatory response	Adenosine receptor A3	Homo sapiens (human)
signal transduction	Adenosine receptor A3	Homo sapiens (human)
activation of adenylate cyclase activity	Adenosine receptor A3	Homo sapiens (human)
regulation of heart contraction	Adenosine receptor A3	Homo sapiens (human)
negative regulation of cell population proliferation	Adenosine receptor A3	Homo sapiens (human)
response to wounding	Adenosine receptor A3	Homo sapiens (human)
regulation of norepinephrine secretion	Adenosine receptor A3	Homo sapiens (human)
negative regulation of cell migration	Adenosine receptor A3	Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activity	Adenosine receptor A3	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	Adenosine receptor A3	Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathway	Adenosine receptor A3	Homo sapiens (human)
synaptic transmission, dopaminergic	Adenosine receptor A2a	Homo sapiens (human)
response to amphetamine	Adenosine receptor A2a	Homo sapiens (human)
regulation of DNA-templated transcription	Adenosine receptor A2a	Homo sapiens (human)
phagocytosis	Adenosine receptor A2a	Homo sapiens (human)
apoptotic process	Adenosine receptor A2a	Homo sapiens (human)
inflammatory response	Adenosine receptor A2a	Homo sapiens (human)
cellular defense response	Adenosine receptor A2a	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
cell-cell signaling	Adenosine receptor A2a	Homo sapiens (human)
synaptic transmission, cholinergic	Adenosine receptor A2a	Homo sapiens (human)
central nervous system development	Adenosine receptor A2a	Homo sapiens (human)
blood coagulation	Adenosine receptor A2a	Homo sapiens (human)
sensory perception	Adenosine receptor A2a	Homo sapiens (human)
locomotory behavior	Adenosine receptor A2a	Homo sapiens (human)
blood circulation	Adenosine receptor A2a	Homo sapiens (human)
negative regulation of cell population proliferation	Adenosine receptor A2a	Homo sapiens (human)
response to xenobiotic stimulus	Adenosine receptor A2a	Homo sapiens (human)
response to inorganic substance	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of glutamate secretion	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmission	Adenosine receptor A2a	Homo sapiens (human)
regulation of norepinephrine secretion	Adenosine receptor A2a	Homo sapiens (human)
response to purine-containing compound	Adenosine receptor A2a	Homo sapiens (human)
response to caffeine	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of synaptic transmission, GABAergic	Adenosine receptor A2a	Homo sapiens (human)
synaptic transmission, glutamatergic	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of urine volume	Adenosine receptor A2a	Homo sapiens (human)
vasodilation	Adenosine receptor A2a	Homo sapiens (human)
eating behavior	Adenosine receptor A2a	Homo sapiens (human)
negative regulation of vascular permeability	Adenosine receptor A2a	Homo sapiens (human)
negative regulation of neuron apoptotic process	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of circadian sleep/wake cycle, sleep	Adenosine receptor A2a	Homo sapiens (human)
negative regulation of alpha-beta T cell activation	Adenosine receptor A2a	Homo sapiens (human)
astrocyte activation	Adenosine receptor A2a	Homo sapiens (human)
neuron projection morphogenesis	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of protein secretion	Adenosine receptor A2a	Homo sapiens (human)
negative regulation of inflammatory response	Adenosine receptor A2a	Homo sapiens (human)
regulation of mitochondrial membrane potential	Adenosine receptor A2a	Homo sapiens (human)
membrane depolarization	Adenosine receptor A2a	Homo sapiens (human)
regulation of calcium ion transport	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Adenosine receptor A2a	Homo sapiens (human)
excitatory postsynaptic potential	Adenosine receptor A2a	Homo sapiens (human)
inhibitory postsynaptic potential	Adenosine receptor A2a	Homo sapiens (human)
prepulse inhibition	Adenosine receptor A2a	Homo sapiens (human)
apoptotic signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of long-term synaptic potentiation	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathway	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of chronic inflammatory response to non-antigenic stimulus	Adenosine receptor A2b	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Adenosine receptor A2b	Homo sapiens (human)
activation of adenylate cyclase activity	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of vascular endothelial growth factor production	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of cGMP-mediated signaling	Adenosine receptor A2b	Homo sapiens (human)
cGMP-mediated signaling	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of chemokine production	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of interleukin-6 production	Adenosine receptor A2b	Homo sapiens (human)
mast cell degranulation	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of mast cell degranulation	Adenosine receptor A2b	Homo sapiens (human)
relaxation of vascular associated smooth muscle	Adenosine receptor A2b	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	Adenosine receptor A2b	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Adenosine receptor A2b	Homo sapiens (human)
vasodilation	Adenosine receptor A2b	Homo sapiens (human)
temperature homeostasis	Adenosine receptor A1	Homo sapiens (human)
response to hypoxia	Adenosine receptor A1	Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathway	Adenosine receptor A1	Homo sapiens (human)
regulation of respiratory gaseous exchange by nervous system process	Adenosine receptor A1	Homo sapiens (human)
negative regulation of acute inflammatory response	Adenosine receptor A1	Homo sapiens (human)
negative regulation of leukocyte migration	Adenosine receptor A1	Homo sapiens (human)
positive regulation of peptide secretion	Adenosine receptor A1	Homo sapiens (human)
positive regulation of systemic arterial blood pressure	Adenosine receptor A1	Homo sapiens (human)
negative regulation of systemic arterial blood pressure	Adenosine receptor A1	Homo sapiens (human)
regulation of glomerular filtration	Adenosine receptor A1	Homo sapiens (human)
protein targeting to membrane	Adenosine receptor A1	Homo sapiens (human)
phagocytosis	Adenosine receptor A1	Homo sapiens (human)
inflammatory response	Adenosine receptor A1	Homo sapiens (human)
signal transduction	Adenosine receptor A1	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Adenosine receptor A1	Homo sapiens (human)
cell-cell signaling	Adenosine receptor A1	Homo sapiens (human)
nervous system development	Adenosine receptor A1	Homo sapiens (human)
negative regulation of cell population proliferation	Adenosine receptor A1	Homo sapiens (human)
response to inorganic substance	Adenosine receptor A1	Homo sapiens (human)
negative regulation of glutamate secretion	Adenosine receptor A1	Homo sapiens (human)
response to purine-containing compound	Adenosine receptor A1	Homo sapiens (human)
lipid catabolic process	Adenosine receptor A1	Homo sapiens (human)
negative regulation of synaptic transmission, GABAergic	Adenosine receptor A1	Homo sapiens (human)
positive regulation of nucleoside transport	Adenosine receptor A1	Homo sapiens (human)
negative regulation of neurotrophin production	Adenosine receptor A1	Homo sapiens (human)
positive regulation of protein dephosphorylation	Adenosine receptor A1	Homo sapiens (human)
vasodilation	Adenosine receptor A1	Homo sapiens (human)
negative regulation of circadian sleep/wake cycle, non-REM sleep	Adenosine receptor A1	Homo sapiens (human)
negative regulation of apoptotic process	Adenosine receptor A1	Homo sapiens (human)
positive regulation of potassium ion transport	Adenosine receptor A1	Homo sapiens (human)
positive regulation of MAPK cascade	Adenosine receptor A1	Homo sapiens (human)
negative regulation of hormone secretion	Adenosine receptor A1	Homo sapiens (human)
cognition	Adenosine receptor A1	Homo sapiens (human)
leukocyte migration	Adenosine receptor A1	Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain	Adenosine receptor A1	Homo sapiens (human)
negative regulation of lipid catabolic process	Adenosine receptor A1	Homo sapiens (human)
positive regulation of lipid catabolic process	Adenosine receptor A1	Homo sapiens (human)
regulation of sensory perception of pain	Adenosine receptor A1	Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergic	Adenosine receptor A1	Homo sapiens (human)
fatty acid homeostasis	Adenosine receptor A1	Homo sapiens (human)
excitatory postsynaptic potential	Adenosine receptor A1	Homo sapiens (human)
long-term synaptic depression	Adenosine receptor A1	Homo sapiens (human)
mucus secretion	Adenosine receptor A1	Homo sapiens (human)
negative regulation of mucus secretion	Adenosine receptor A1	Homo sapiens (human)
triglyceride homeostasis	Adenosine receptor A1	Homo sapiens (human)
regulation of cardiac muscle cell contraction	Adenosine receptor A1	Homo sapiens (human)
apoptotic signaling pathway	Adenosine receptor A1	Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration	Adenosine receptor A1	Homo sapiens (human)
negative regulation of long-term synaptic potentiation	Adenosine receptor A1	Homo sapiens (human)
negative regulation of long-term synaptic depression	Adenosine receptor A1	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Adenosine receptor A1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
G protein-coupled adenosine receptor activity	Adenosine receptor A3	Homo sapiens (human)
G protein-coupled adenosine receptor activity	Adenosine receptor A2a	Homo sapiens (human)
protein binding	Adenosine receptor A2a	Homo sapiens (human)
calmodulin binding	Adenosine receptor A2a	Homo sapiens (human)
lipid binding	Adenosine receptor A2a	Homo sapiens (human)
enzyme binding	Adenosine receptor A2a	Homo sapiens (human)
type 5 metabotropic glutamate receptor binding	Adenosine receptor A2a	Homo sapiens (human)
identical protein binding	Adenosine receptor A2a	Homo sapiens (human)
protein-containing complex binding	Adenosine receptor A2a	Homo sapiens (human)
alpha-actinin binding	Adenosine receptor A2a	Homo sapiens (human)
G protein-coupled adenosine receptor activity	Adenosine receptor A2b	Homo sapiens (human)
protein binding	Adenosine receptor A2b	Homo sapiens (human)
G protein-coupled receptor activity	Adenosine receptor A2b	Homo sapiens (human)
G protein-coupled receptor binding	Adenosine receptor A1	Homo sapiens (human)
purine nucleoside binding	Adenosine receptor A1	Homo sapiens (human)
protein binding	Adenosine receptor A1	Homo sapiens (human)
heat shock protein binding	Adenosine receptor A1	Homo sapiens (human)
G-protein beta/gamma-subunit complex binding	Adenosine receptor A1	Homo sapiens (human)
heterotrimeric G-protein binding	Adenosine receptor A1	Homo sapiens (human)
protein heterodimerization activity	Adenosine receptor A1	Homo sapiens (human)
G protein-coupled adenosine receptor activity	Adenosine receptor A1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Adenosine receptor A3	Homo sapiens (human)
presynaptic membrane	Adenosine receptor A3	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Adenosine receptor A3	Homo sapiens (human)
dendrite	Adenosine receptor A3	Homo sapiens (human)
plasma membrane	Adenosine receptor A3	Homo sapiens (human)
synapse	Adenosine receptor A3	Homo sapiens (human)
plasma membrane	Adenosine receptor A2a	Homo sapiens (human)
intermediate filament	Adenosine receptor A2a	Homo sapiens (human)
plasma membrane	Adenosine receptor A2a	Homo sapiens (human)
membrane	Adenosine receptor A2a	Homo sapiens (human)
dendrite	Adenosine receptor A2a	Homo sapiens (human)
axolemma	Adenosine receptor A2a	Homo sapiens (human)
asymmetric synapse	Adenosine receptor A2a	Homo sapiens (human)
presynaptic membrane	Adenosine receptor A2a	Homo sapiens (human)
neuronal cell body	Adenosine receptor A2a	Homo sapiens (human)
postsynaptic membrane	Adenosine receptor A2a	Homo sapiens (human)
presynaptic active zone	Adenosine receptor A2a	Homo sapiens (human)
glutamatergic synapse	Adenosine receptor A2a	Homo sapiens (human)
plasma membrane	Adenosine receptor A2b	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Adenosine receptor A2b	Homo sapiens (human)
presynapse	Adenosine receptor A2b	Homo sapiens (human)
glutamatergic synapse	Adenosine receptor A2b	Homo sapiens (human)
plasma membrane	Adenosine receptor A2b	Homo sapiens (human)
plasma membrane	Adenosine receptor A1	Homo sapiens (human)
plasma membrane	Adenosine receptor A1	Homo sapiens (human)
basolateral plasma membrane	Adenosine receptor A1	Homo sapiens (human)
axolemma	Adenosine receptor A1	Homo sapiens (human)
asymmetric synapse	Adenosine receptor A1	Homo sapiens (human)
presynaptic membrane	Adenosine receptor A1	Homo sapiens (human)
neuronal cell body	Adenosine receptor A1	Homo sapiens (human)
terminal bouton	Adenosine receptor A1	Homo sapiens (human)
dendritic spine	Adenosine receptor A1	Homo sapiens (human)
calyx of Held	Adenosine receptor A1	Homo sapiens (human)
postsynaptic membrane	Adenosine receptor A1	Homo sapiens (human)
presynaptic active zone	Adenosine receptor A1	Homo sapiens (human)
synapse	Adenosine receptor A1	Homo sapiens (human)
dendrite	Adenosine receptor A1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (35)

Assay ID	Title	Year	Journal	Article
AID1138025	Inhibition of human recombinant adenosine A3 receptor	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1138020	Selectivity ratio of Ki for human recombinant adenosine A1 receptor to Ki for human recombinant adenosine receptor A2a	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID412521	Half life in Sprague-Dawley rat at 2 mg/kg, iv	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412528	Increase in locomotor activity in mouse at 100 mg/kg administered for 4 days	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412527	Toxicity in mouse at 100 mg/kg administered for 4 days	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412534	Antagonist activity at human adenosine A3 receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID1871328	Antagonist activity at adenosine A2A receptor (unknown origin)	2022	European journal of medicinal chemistry, Jan-05, Volume: 227	Adenosine receptor antagonists: Recent advances and therapeutic perspective.
AID412532	Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412504	Displacement of radioligand from human recombinant adenosine A1 receptor at 21 degC after 90 mins by cell-based microplate scintillation counting	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412523	Drug uptake in Sprague-Dawley rat brain at 2 mg/kg, iv	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID1907398	Displacement of [3H]SCH5826 from human A2AAR incubated for 60 mins by scintillation counter analysis	2022	European journal of medicinal chemistry, Jun-05, Volume: 236	Dual-acting antitumor agents targeting the A
AID412520	Apparent permeability across human Caco-2 cell membrane	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412536	Binding affinity to human adenosine A1 receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412524	Tmax in Sprague-Dawley rat at 2 mg/kg, iv	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID1138021	Inhibition of human recombinant adenosine receptor A2b	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID412533	Antagonist activity at human adenosine A1 receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412538	Binding affinity to human adenosine A3 receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID1138023	Inhibition of human recombinant adenosine receptor A2a	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1138039	Selectivity ratio of Ki for human recombinant adenosine A3 receptor to Ki for human recombinant adenosine receptor A2a	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1138024	Inhibition of human recombinant adenosine A1 receptor	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID412503	Displacement of radioligand from human recombinant adenosine A2A receptor at 21 degC after 90 mins by cell-based microplate scintillation counting	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412526	Toxicity in mouse L5178Y cells assessed as nonmutagenic activity	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412535	Binding affinity to human adenosine A2A receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412525	Binding affinity to human ERG at 30 uM by patch clamp technique	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412505	Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID1138063	Anticataleptic activity in rat assessed as minimum efficacious dose	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID412506	Displacement of radioligand from human recombinant adenosine A3 receptor at 21 degC after 60 mins by cell-based microplate scintillation counting	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412522	Oral bioavailability in Sprague-Dawley rat	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID412537	Binding affinity to human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID1138036	Selectivity ratio of Ki for human recombinant adenosine receptor A2b to Ki for human recombinant adenosine receptor A2a	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID412518	Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assay	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID1345822	Human A3 receptor (Adenosine receptors)	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID1345721	Human A2B receptor (Adenosine receptors)	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID1345685	Human A1 receptor (Adenosine receptors)	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
AID1345618	Human A2A receptor (Adenosine receptors)	2009	Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1	Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	2 (40.00)	29.6817
2010's	1 (20.00)	24.3611
2020's	2 (40.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	1 (16.67%)	5.53%
Reviews	3 (50.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	2 (33.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
adenine [no description available]	3.14	1	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
enprofylline enprofylline : Xanthine bearing a propyl substituent at position 3. A bronchodilator, it is used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy.	3.51	1	oxopurine	anti-arrhythmia drug; anti-asthmatic drug; bronchodilator agent; non-steroidal anti-inflammatory drug
theophylline [no description available]	4.19	2	dimethylxanthine	adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent
caffeine [no description available]	4.19	2	purine alkaloid; trimethylxanthine	adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic
cgs 15943 9-chloro-2-(2-furyl)-(1,2,4)triazolo(1,5-c)quinazolin-5-imine: non-xanthine triazoloquinazoline adenosine antagonist. CGS 15943 : A member of the class of triazoloquinazolines that is [1,2,4]triazolo[1,5-c]quinazoline substited at positions 2, 5 and 9 by furan-2-yl, amino and chloro groups respectively. A potent antagonist at adenosine A1 and adenosine A2A receptors.	3.19	1	aromatic amine; biaryl; furans; organochlorine compound; primary amino compound; quinazolines; triazoloquinazoline	adenosine A1 receptor antagonist; adenosine A2A receptor antagonist; antineoplastic agent; central nervous system stimulant
vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).	2.41	1	dicarboxylic acid diamide; hydroxamic acid	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor
levodopa Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease	3.51	1	amino acid zwitterion; dopa; L-tyrosine derivative; non-proteinogenic L-alpha-amino acid	allelochemical; antidyskinesia agent; antiparkinson drug; dopaminergic agent; hapten; human metabolite; mouse metabolite; neurotoxin; plant growth retardant; plant metabolite; prodrug
2-chloroadenosine 5-chloroformycin A: structure given in first source	3.19	1	purine nucleoside
adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit	3.19	1	adenosines; purines D-ribonucleoside	analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent
rolofylline rolofylline: selective antagonist for adenosine receptors; a cardiovascular agent	3.51	1	oxopurine
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	3.14	1	1,2,3-triazole
zm 241385 ZM 241385: a high affinity radioligand selective for the A2a adenosine receptor	4.19	2	diamino-1,3,5-triazine
sch 58261 [no description available]	4.19	2	triazolopyrimidines
regadenoson [no description available]	3.19	1	purine nucleoside
adenosine-5'-(n-ethylcarboxamide) Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.. N-ethyl-5'-carboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by an N-ethylcarboxamido group.	3.19	1	adenosines; monocarboxylic acid amide	adenosine A1 receptor agonist; adenosine A2A receptor agonist; antineoplastic agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent
wr-142,490 (+)-(11R,2'S)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (+)-(11R,2'S)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.	3.19	1	[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol	antimalarial
2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-n-ethylcarboxamidoadenosine 2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-N-ethylcarboxamidoadenosine: structure given in first source	3.19	1
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine 2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine: A2 adenosine receptor agonist; structure given in first source. CGS-21680 : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by N-ethylcarboxamido and the hydrogen at position 2 on the adenine is replaced by a 4-(2-carboxyethyl)phenethylamino group.	4.19	2	adenosines; dicarboxylic acid monoamide; monocarboxylic acid	adenosine A2A receptor agonist; anti-inflammatory agent
mrs 1523 2,3-diethyl-4,5-dipropyl-6-phenylpyridine-3-thiocarboxylate-5-carboxylate: adenosine A3 receptor antagonist	3.51	1
istradefylline [no description available]	4.41	3	oxopurine
mrs 1754 [no description available]	3.51	1	oxopurine
cv 1808 2-phenylaminoadenosine: has coronary & cardiohemodynamic effects	3.19	1	purine nucleoside
1-(3,4-dichlorophenyl)-3-(4-((1-ethyl-3-piperidyl)amino)-6-methyl-2-pyrimidinyl)guanidine 1-(3,4-dichlorophenyl)-3-(4-((1-ethyl-3-piperidyl)amino)-6-methyl-2-pyrimidinyl)guanidine: structure	3.51	1
binodenoson [no description available]	3.19	1
atl 146e BMS-068645: structure in first source	3.19	1
st 1535 [no description available]	3.19	1
mocetinostat mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).	2.41	1	aminopyrimidine; benzamides; pyridines; secondary amino compound; secondary carboxamide; substituted aniline	antineoplastic agent; apoptosis inducer; autophagy inducer; cardioprotective agent; EC 3.5.1.98 (histone deacetylase) inhibitor; hepatotoxic agent
2-(2-(4-chlorophenyl)ethoxy)adenosine 2-(2-(4-chlorophenyl)ethoxy)adenosine: a adenosine A2A receptor agonist	3.19	1
2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-7h-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidine-5-amine [no description available]	4.19	2
tozadenant tozadenant: an adenosine A2A receptor antagonist	4.19	2	benzothiazoles
psb 36 1-butyl-8-(3-noradamantyl)-3-(3-hydroxypropyl)xanthine: an A1 receptor antagonist	3.51	1	oxopurine
psb603 PSB603: an adenosine A2B receptor antagonist	3.51	1
psb 11 [no description available]	3.51	1
n-benzo(1,3)dioxol-5-yl-2-(5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1h-purin-8-yl)-1-methyl-1h-pyrazol-3-yloxy)-acetamide [no description available]	3.51	1

Condition	Indicated	Relationship Strength	Studies
Ambulation Disorders, Neurologic [description not available]	0	2.05	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.96	1
Idiopathic Parkinson Disease [description not available]	0	2.96	1
Parkinson Disease A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)	1	4.96	1

v 2006

Description

Cross-References

Synonyms (55)

Protein Targets (4)

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (105)

Molecular Functions (16)

Ceullar Components (18)

Bioassays (35)

Research

Studies (5)

Market Indicators

Research Demand Index: 24.51

Study Types

v 2006

Description

Cross-References

Synonyms (55)

Protein Targets (4)

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (105)

Molecular Functions (16)

Ceullar Components (18)

Bioassays (35)

Research

Studies (5)

Market Indicators

Research Demand Index: 24.51

Study Types

Related Drugs (34)

Related Conditions (4)