Page last updated: 2024-11-13

mrs2500

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 CID44448831
CHEMBL ID444278
SCHEMBL ID19807535
MeSH IDM0479809

Synonyms (17)

Synonym
[(1r,2s,4s,5s)-4-[2-iodo-6-(methylamino)purin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphate
gtpl1724
mrs2500
mrs 2500
mrs-2500
CHEMBL444278 ,
bdbm50373326
[(1r,2s,4s,5s)-4-[2-iodo-6-(methylamino)-9h-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hex-1-yl]methyl dihydrogen phosphate
2id ,
SCHEMBL19807535
Q27087776
((1r,2s,4s,5s)-4-(2-iodo-6-(methylamino)-9h-purin-9-yl)-2-(phosphonooxy)bicyclo(3.1.0)hex-1-yl)methyl dihydrogen phosphate
unii-dwq8uhz38s
bicyclo(3.1.0)hexane-1-methanol, 4-(2-iodo-6-(methylamino)-9h-purin-9-yl)-2-(phosphonooxy)-, dihydrogen phosphate (ester), (1r,2s,4s,5s)-
dwq8uhz38s ,
bicyclo(3.1.0)hexane-1-methanol, 4-(2-iodo-6-(methylamino)-9h-purin-9-yl)-2-(phosphonooxy)-, 1-(dihydrogen phosphate), (1r,2s,4s,5s)-
AKOS040746133
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
P2Y purinoceptor 1Homo sapiens (human)IC50 (µMol)0.00840.00840.48313.0000AID150334
P2Y purinoceptor 1Homo sapiens (human)Ki0.00080.00080.00080.0008AID1421250; AID150336; AID319605
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (31)

Processvia Protein(s)Taxonomy
positive regulation of protein phosphorylationP2Y purinoceptor 1Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
monoatomic ion transportP2Y purinoceptor 1Homo sapiens (human)
cell surface receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationP2Y purinoceptor 1Homo sapiens (human)
glial cell migrationP2Y purinoceptor 1Homo sapiens (human)
regulation of cell shapeP2Y purinoceptor 1Homo sapiens (human)
response to mechanical stimulusP2Y purinoceptor 1Homo sapiens (human)
negative regulation of norepinephrine secretionP2Y purinoceptor 1Homo sapiens (human)
signal transduction involved in regulation of gene expressionP2Y purinoceptor 1Homo sapiens (human)
platelet activationP2Y purinoceptor 1Homo sapiens (human)
positive regulation of inositol trisphosphate biosynthetic processP2Y purinoceptor 1Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 1Homo sapiens (human)
eating behaviorP2Y purinoceptor 1Homo sapiens (human)
positive regulation of monoatomic ion transportP2Y purinoceptor 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIP2Y purinoceptor 1Homo sapiens (human)
positive regulation of hormone secretionP2Y purinoceptor 1Homo sapiens (human)
establishment of localization in cellP2Y purinoceptor 1Homo sapiens (human)
positive regulation of penile erectionP2Y purinoceptor 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeP2Y purinoceptor 1Homo sapiens (human)
response to growth factorP2Y purinoceptor 1Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 1Homo sapiens (human)
cellular response to purine-containing compoundP2Y purinoceptor 1Homo sapiens (human)
protein localization to plasma membraneP2Y purinoceptor 1Homo sapiens (human)
relaxation of muscleP2Y purinoceptor 1Homo sapiens (human)
blood vessel diameter maintenanceP2Y purinoceptor 1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationP2Y purinoceptor 1Homo sapiens (human)
regulation of synaptic vesicle exocytosisP2Y purinoceptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
G protein-coupled ADP receptor activityP2Y purinoceptor 1Homo sapiens (human)
protein bindingP2Y purinoceptor 1Homo sapiens (human)
ATP bindingP2Y purinoceptor 1Homo sapiens (human)
signaling receptor activityP2Y purinoceptor 1Homo sapiens (human)
ADP bindingP2Y purinoceptor 1Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 1Homo sapiens (human)
G protein-coupled ATP receptor activityP2Y purinoceptor 1Homo sapiens (human)
protein heterodimerization activityP2Y purinoceptor 1Homo sapiens (human)
scaffold protein bindingP2Y purinoceptor 1Homo sapiens (human)
A1 adenosine receptor bindingP2Y purinoceptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
plasma membraneP2Y purinoceptor 1Homo sapiens (human)
ciliumP2Y purinoceptor 1Homo sapiens (human)
cell surfaceP2Y purinoceptor 1Homo sapiens (human)
postsynaptic densityP2Y purinoceptor 1Homo sapiens (human)
basolateral plasma membraneP2Y purinoceptor 1Homo sapiens (human)
apical plasma membraneP2Y purinoceptor 1Homo sapiens (human)
dendriteP2Y purinoceptor 1Homo sapiens (human)
cell bodyP2Y purinoceptor 1Homo sapiens (human)
postsynaptic membraneP2Y purinoceptor 1Homo sapiens (human)
presynaptic active zone membraneP2Y purinoceptor 1Homo sapiens (human)
glutamatergic synapseP2Y purinoceptor 1Homo sapiens (human)
plasma membraneP2Y purinoceptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID1465404Selectivity ratio of IC50 for P2Y2 receptor Y306F mutant (unknown origin) to IC50 for wild type P2Y2 receptor (unknown origin)2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y
AID319605Binding affinity to human P2Y1 receptor2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
P2Y1 receptor antagonists as novel antithrombotic agents.
AID150334Antagonistic activity against P2Y purinoceptor 12003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.
AID1465403Selectivity ratio of IC50 for P2Y2 receptor Y303F mutant (unknown origin) to IC50 for wild type P2Y2 receptor (unknown origin)2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y
AID1421250Displacement of [3H]2-chloro-N 6- methyl-( N )-methanocarba-2'-deoxyadenosine 3 '5 '-bis-phosphate from human P2Y1 expressed in baculovirus infected insect Sf9 cells after 30 mins by scintillation spectrometric method2018European journal of medicinal chemistry, Oct-05, Volume: 158Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y
AID1465402Selectivity ratio of IC50 for P2Y2 receptor A286W mutant (unknown origin) to IC50 for wild type P2Y2 receptor (unknown origin)2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y
AID1465400Selectivity ratio of IC50 for P2Y2 receptor K46A mutant (unknown origin) to IC50 for wild type P2Y2 receptor (unknown origin)2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y
AID1465401Selectivity ratio of IC50 for P2Y2 receptor R195A mutant (unknown origin) to IC50 for wild type P2Y2 receptor (unknown origin)2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y
AID150336Inhibition of [3H]5 binding to P2Y purinoceptor 1 expressed in Sf9 cells2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.
AID1346309Human P2Y1 receptor (P2Y receptors)2004Biochemical pharmacology, Nov-15, Volume: 68, Issue:10
Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor.
AID1346309Human P2Y1 receptor (P2Y receptors)2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (60.00)29.6817
2010's2 (40.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.39

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 Index25.39 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.42 (4.65)
Search Engine Demand Index20.59 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.39)

All Compounds (24.57)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]