Page last updated: 2024-12-07

methylthio-adp

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 CID121990
CHEMBL ID435402
SCHEMBL ID195864
MeSH IDM0043083

Synonyms (26)

Synonym
gtpl1763
[3h]2mesadp
[3h]2-methylthio-adp
gtpl1710
2-methylthio-adenosine-5'-diphosphate
2mesadp
2-mesadp
methylthio-adp
2-(methylthio)-adenosinediphosphate
CHEMBL435402 ,
((2r,3s,4r,5r)-5-(6-amino-2-(methylthio)-9h-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl trihydrogen diphosphate
bdbm50118242
[({[(2r,3s,4r,5r)-5-[6-amino-2-(methylsulfanyl)-9h-purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxy}(hydroxy)phosphoryl)oxy]phosphonic acid
((2s,3r,4s,5s)-5-(6-amino-2-(methylthio)-9h-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl trihydrogen diphosphate
[(2r,3s,4r,5r)-5-(6-amino-2-methylsulfanylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphono hydrogen phosphate
adenosine 5'-(trihydrogen diphosphate), 2-(methylthio)-
34983-48-7
(3h)2-mes-adp
6ad ,
2-(methylsulfanyl)adenosine 5'-(trihydrogen diphosphate)
SCHEMBL195864
2-(methylthio)adenosine 5'-diphosphate
Q27072021
DTXSID20956439
9-{5-o-[hydroxy(phosphonooxy)phosphoryl]pentofuranosyl}-2-(methylsulfanyl)-9h-purin-6-amine
((2r,3s,4r,5r)-5-(6-amino-2-(methylthio)-9h-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyltrihydrogendiphosphate

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Despite its moderate bioavailability in rats, oral administration of SAR216471 resulted in a fast, potent, and sustained inhibition of platelet aggregation where the extent and duration of platelet inhibition were directly proportional to its circulating plasma levels."( SAR216471, an alternative to the use of currently available P2Y₁₂ receptor inhibitors?
Boldron, C; Bonnet-Lignon, S; Bono, F; Delesque-Touchard, N; Herbert, JM; Lassalle, G; Millet, L; Pflieger, AM; Salel, V; Savi, P, 2014
)
0.4

Dosage Studied

ExcerptRelevanceReference
" Bell-shaped dose-response curves for stimulation of phosphoinositide hydrolysis were obtained in these cells."( Dual effect of nucleotides on P2Y receptors.
Barnard, EA; Järv, J; Sak, K, 2000
)
0.31
" The dose-response curve was shifted to the left in both cases, suggesting increased MK reactivity."( Acetylsalicylic acid enhances purinergic receptor-mediated outward currents in rat megakaryocytes.
Beckerman, J; Myers, A; Vicini, S; Young, JP, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Ectonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)Ki23.52000.52003.93508.1900AID1415776; AID1415777; AID1415778; AID1415779
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)0.04000.00002.398310.0000AID242671
P2Y purinoceptor 1Homo sapiens (human)IC50 (µMol)1.55090.00840.48313.0000AID242607; AID242669; AID242670; AID242671; AID242672; AID242673; AID242698
P2Y purinoceptor 12Homo sapiens (human)Ki0.03210.00202.82209.8300AID1850681
[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)
P2Y purinoceptor 2Homo sapiens (human)EC50 (µMol)100.00000.00560.682810.0000AID150321
P2Y purinoceptor 1Homo sapiens (human)EC50 (µMol)8.32190.00130.42027.2000AID1256110; AID150330; AID165066; AID165067; AID165068; AID165069; AID165070; AID165071; AID165072; AID165073; AID165074; AID165075; AID165076; AID165077; AID165078; AID165079; AID165080; AID165081; AID165082; AID165083; AID165084; AID165085; AID165086; AID165087; AID165088; AID165089; AID165090; AID165091; AID240230; AID240279; AID240280; AID240281; AID240282; AID240283; AID240294; AID240297; AID240321; AID240322; AID240323; AID240324; AID240325; AID240326; AID240327; AID240328; AID240329; AID240330; AID240331; AID240332; AID240333; AID240334; AID240335; AID240336; AID240337; AID240338; AID240339; AID240340; AID240341; AID240342; AID240343; AID240344; AID240345; AID240346; AID240347; AID240348; AID240349; AID240350; AID240351; AID240352; AID240353; AID240354; AID240355; AID240356; AID240357; AID240358; AID240359; AID240392; AID261698; AID302988; AID462461; AID462811; AID751213
P2Y purinoceptor 1Rattus norvegicus (Norway rat)EC50 (µMol)0.10000.00100.05370.1000AID261696
P2Y purinoceptor 1Meleagris gallopavo (turkey)EC50 (µMol)0.00420.00251.70498.0000AID150470; AID165252; AID373705; AID475246; AID647893; AID705929
[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)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (84)

Processvia Protein(s)Taxonomy
generation of precursor metabolites and energyEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
phosphate-containing compound metabolic processEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
immune responseEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
nucleoside triphosphate catabolic processEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
response to inorganic substanceEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
gene expressionEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
vesicle-mediated transportEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
bone mineralizationEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
negative regulation of cell growthEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
melanocyte differentiationEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
regulation of bone mineralizationEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
negative regulation of bone mineralizationEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
inorganic diphosphate transportEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
intracellular phosphate ion homeostasisEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
sequestering of triglycerideEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
negative regulation of protein autophosphorylationEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
cellular response to insulin stimulusEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
response to ATPEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
negative regulation of fat cell differentiationEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
negative regulation of glycogen biosynthetic processEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
ATP metabolic processEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
negative regulation of glucose importEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
negative regulation of insulin receptor signaling pathwayEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
3'-phosphoadenosine 5'-phosphosulfate metabolic processEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
phosphate ion homeostasisEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
nucleic acid metabolic processEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
negative regulation of hh target transcription factor activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
intracellular monoatomic ion homeostasisP2Y purinoceptor 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
positive regulation of mucus secretionP2Y purinoceptor 2Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 2Homo sapiens (human)
blood vessel diameter maintenanceP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 2Homo sapiens (human)
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)
G protein-coupled adenosine receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
monoatomic ion transportP2Y purinoceptor 12Homo sapiens (human)
substrate-dependent cell migration, cell extensionP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
hemostasisP2Y purinoceptor 12Homo sapiens (human)
calcium-mediated signalingP2Y purinoceptor 12Homo sapiens (human)
cerebral cortex radial glia-guided migrationP2Y purinoceptor 12Homo sapiens (human)
cell projection organizationP2Y purinoceptor 12Homo sapiens (human)
lamellipodium assemblyP2Y purinoceptor 12Homo sapiens (human)
platelet activationP2Y purinoceptor 12Homo sapiens (human)
positive regulation of integrin activation by cell surface receptor linked signal transductionP2Y purinoceptor 12Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
positive regulation of monoatomic ion transportP2Y purinoceptor 12Homo sapiens (human)
response to axon injuryP2Y purinoceptor 12Homo sapiens (human)
regulation of chemotaxisP2Y purinoceptor 12Homo sapiens (human)
positive regulation of chemotaxisP2Y purinoceptor 12Homo sapiens (human)
establishment of localization in cellP2Y purinoceptor 12Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionP2Y purinoceptor 12Homo sapiens (human)
platelet aggregationP2Y purinoceptor 12Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 12Homo sapiens (human)
visual system developmentP2Y purinoceptor 12Homo sapiens (human)
positive regulation of ruffle assemblyP2Y purinoceptor 12Homo sapiens (human)
regulation of microglial cell migrationP2Y purinoceptor 12Homo sapiens (human)
positive regulation of microglial cell migrationP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (45)

Processvia Protein(s)Taxonomy
nucleic acid bindingEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
exonuclease activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
phosphodiesterase I activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
dinucleotide phosphatase activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
scavenger receptor activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
insulin receptor bindingEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
calcium ion bindingEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
protein bindingEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
ATP bindingEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
zinc ion bindingEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
phosphatase activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
polysaccharide bindingEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
GTP diphosphatase activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
UTP diphosphatase activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
protein homodimerization activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
nucleoside triphosphate diphosphatase activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
ATP diphosphatase activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
3'-phosphoadenosine 5'-phosphosulfate bindingEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
cyclic-GMP-AMP hydrolase activityEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
protein bindingP2Y purinoceptor 2Homo sapiens (human)
signaling receptor activityP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 2Homo sapiens (human)
A1 adenosine receptor bindingP2Y purinoceptor 2Homo sapiens (human)
G protein-coupled UTP receptor activityP2Y purinoceptor 2Homo sapiens (human)
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)
G protein-coupled adenosine receptor activityP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled ADP receptor activityP2Y purinoceptor 12Homo sapiens (human)
guanyl-nucleotide exchange factor activityP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
plasma membraneEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
extracellular spaceEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
lysosomal membraneEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
plasma membraneEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
cell surfaceEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
membraneEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
basolateral plasma membraneEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
cell surfaceEctonucleotide pyrophosphatase/phosphodiesterase family member 1Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
plasma membraneP2Y purinoceptor 2Homo sapiens (human)
plasma membraneP2Y purinoceptor 2Homo sapiens (human)
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)
plasma membraneP2Y purinoceptor 12Homo sapiens (human)
cell surfaceP2Y purinoceptor 12Homo sapiens (human)
membraneP2Y purinoceptor 12Homo sapiens (human)
cell projection membraneP2Y purinoceptor 12Homo sapiens (human)
cell body membraneP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (139)

Assay IDTitleYearJournalArticle
AID165068Compound was measured for the antagonism of the activation of phospholipase C in mutant(F226A) human P2Y1 receptor in presence of MRS2179.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID751212Agonist activity at human GFP-tagged P2Y11R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay2013Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12
Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists.
AID240230Effective concentration to activate wild-type P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165252Activation of Purinoceptor P2Y1-mediated phospholipase C in turkey erythrocyte membranes2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.
AID240281Effective concentration to activate human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID150470Evaluated for agonist activity against phospholipase C coupled P2Y purinoceptor 1 (P2Y1) of turkey erythrocytes2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Purine and pyrimidine (P2) receptors as drug targets.
AID162990Relative half maximal velocity of Pyruvate kinase and Phosphoenolpyruvate1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID240328Effective concentration required for the activation of human D289A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240339Effective concentration required for the activation of human K196A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165080Compound was measured for the antagonism of the activation of phospholipase C in mutant(S314T) human P2Y1 receptor in presence of MRS21791998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID240353Effective concentration required for the activation of human R310K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID227598Ratio of Km(ADP)/Ki or Km for rat muscle pyruvate kinase1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID240297Effective concentration to activate human Y203A (EL2) mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165091Compound was measured for the antagonism of the activation of phospholipase C in mutant(Y136A) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID165089Compound was measured for the antagonism of the activation of phospholipase C in mutant(WT) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID705934Stability of the compound assessed as human eNPP1-mediated degradation of compound measuring increase in NMP level at pH 8.5 at 0.2 mM after 20 mins by HPLC relative to control2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist.
AID261697Activity against rat P2Y2-GFP transfected in HEK293 cells by intracellular calcium increase2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors.
AID1415779Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using p-Nph-5'-AMP as substrate after 30 mins by capillary electrophoresis method2017MedChemComm, May-01, Volume: 8, Issue:5
Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors.
AID240342Effective concentration required for the activation of human Q307A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID1465390Selectivity ratio of EC50 for P2Y2 receptor K46A mutant (unknown origin) to EC50 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
AID240357Effective concentration required for the activation of human T221A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165081Compound was measured for the antagonism of the activation of phospholipase C in mutant(S314T) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID240329Effective concentration required for the activation of human D300A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240350Effective concentration required for the activation of human R287Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID462461Activation of human P2Y1 receptor expressed in human 1321N1 cells assessed as induction of calcium flux by FLIPR assay2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Structure-activity relationship of (N)-Methanocarba phosphonate analogues of 5'-AMP as cardioprotective agents acting through a cardiac P2X receptor.
AID240324Effective concentration required for the activation of human D204A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID462821Stability in human serum assessed as half life of hydrolysis2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
A novel insulin secretagogue based on a dinucleoside polyphosphate scaffold.
AID475246Agonist activity at turkey P2Y1 receptor expressed in human 132N1 receptor assessed as induction of intracellular calcium mobilization2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
2-MeS-beta,gamma-CCl2-ATP is a potent agent for reducing intraocular pressure.
AID165085Compound was measured for the antagonism of the activation of phospholipase C in mutant(T221A) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID234672Relative inhibitory potency as ratio of kidney and liver pyruvate kinases1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID150330Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.
AID647893Agonist activity at turkey P2Y purinoceptor 1 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Boranophosphate isoster controls P2Y-receptor subtype selectivity and metabolic stability of dinucleoside polyphosphate analogues.
AID240279Effective concentration to activate human Y203F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID163119Relative half maximal velocity of Pyruvate kinase and Phosphoenolpyruvate1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID240283Effective concentration to activate human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240294Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID462811Agonist activity at G-protein coupled P2Y1 receptor expressed in human 1321N1 cells assessed as increase in calcium by Fura2 assay2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
A novel insulin secretagogue based on a dinucleoside polyphosphate scaffold.
AID165072Compound was measured for the antagonism of the activation of phospholipase C in mutant(H277A) human P2Y1 receptor in presence of MRS21791998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID1465393Selectivity ratio of EC50 for P2Y2 receptor Y303F mutant (unknown origin) to EC50 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
AID240334Effective concentration required for the activation of human F131A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID705925Half life in human serum at 40 mM by HPLC2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist.
AID165090Compound was measured for the antagonism of the activation of phospholipase C in mutant(Y136A) human P2Y1 receptor in presence of MRS2179 (P<0.005)1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID240341Effective concentration required for the activation of human K280A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID242698Inhibition concentration required against human Y203A (EL2) mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240326Effective concentration required for the activation of human D204N mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID70544Agonism at turkey erythrocyte P2Y receptor.1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate.
AID240352Effective concentration required for the activation of human R310A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID162978Michaelis-Menten constant for inhibition of rat kidney pyruvate kinase (PK-K)1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID165073Compound was measured for the antagonism of the activation of phospholipase C in mutant(H277A) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID240331Effective concentration required for the activation of human E209D mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID705933Half life in Tris buffer at pH 9.8 at 0.2 mg by HPLC in presence of alkaline phosphatase2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist.
AID240280Effective concentration to activate human Y273A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165075Compound was measured for the antagonism of the activation of phospholipase C in mutant(K280A) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID165078Compound was measured for the antagonism of the activation of phospholipase C in mutant(R310K) human P2Y1 receptor in presence of MRS21791998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID240282Effective concentration to activate human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240336Effective concentration required for the activation of human H132A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID1256111Agonist activity at GFP-tagged human P2Y11R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5'-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action.
AID302988Agonist activity at P2Y1 receptor expressed in 1321N1 cells assessed as cytosolic calcium level2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
New iantherans from the marine sponge Ianthella quadrangulata: novel agonists of the P2Y(11) receptor.
AID240327Effective concentration required for the activation of human D208A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240358Effective concentration required for the activation of human T222A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240335Effective concentration required for the activation of human F226A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165088Compound was measured for the antagonism of the activation of phospholipase C in mutant(WT) human P2Y1 receptor in presence of MRS2179 (P<0.005)1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID167874Tested for relaxation of carbachol-contracted rabbit aorta at 37 degree C; Significantly more potent than 2MeSATP1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate.
AID165079Compound was measured for the antagonism of the activation of phospholipase C in mutant(R310K) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID165086Compound was measured for the antagonism of the activation of phospholipase C in mutant(T222A) human P2Y1 receptor in presence of MRS2179 (P<0.005)1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID261698Activity against human P2Y1-GFP expressed in 1321N1 cells by intracellular calcium increase2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors.
AID240344Effective concentration required for the activation of human R195A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID242673Inhibition concentration required against human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165071Compound was measured for the antagonism of the activation of phospholipase C in mutant(H132A) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID240323Effective concentration required for the activation of human C296A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID150623Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2r; No effect as either agonist or antagonist at 10 uM2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.
AID240354Effective concentration required for the activation of human S314A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240392Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate is determined in separate experiment2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165066Compound was measured for the antagonism of the activation of phospholipase C in mutant(F131A) human P2Y1 receptor in presence of MRS2179 (P<0.05)1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID227596Ratio of Km(ADP)/Ki or Km for rat liver pyruvate kinase1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID240348Effective concentration required for the activation of human R287E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240340Effective concentration required for the activation of human K198A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240346Effective concentration required for the activation of human R285A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240345Effective concentration required for the activation of human R212A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240333Effective concentration required for the activation of human E209R mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID242670Inhibition concentration required against human Y273A mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]-MRS2279 as radioligand2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID1465392Selectivity ratio of EC50 for P2Y2 receptor A286W mutant (unknown origin) to EC50 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
AID240321Effective concentration required for the activation of human C124A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID1465391Selectivity ratio of EC50 for P2Y2 receptor R195A mutant (unknown origin) to EC50 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
AID1256110Agonist activity at GFP-tagged human P2Y1R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5'-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action.
AID234673Relative inhibitory potency as ratio of muscle and liver pyruvate kinases1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID240325Effective concentration required for the activation of human D204E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165082Compound was measured for the antagonism of the activation of phospholipase C in mutant(S317A) human P2Y1 receptor in presence of MRS21791998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID162985Michaelis-Menten constant for inhibition of pyruvate kinase obtained from rat liver (PK-L) was determined using ADP as competitive inhibitor1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID150630Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 4; No effect as either agonist or antagonist at 10 uM2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.
AID165084Compound was measured for the antagonism of the activation of phospholipase C in mutant(T221A) human P2Y1 receptor in presence of MRS2179 (P<0.005)1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID240351Effective concentration required for the activation of human R301A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID1415776Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using ATP as substrate by capillary electrophoresis method2017MedChemComm, May-01, Volume: 8, Issue:5
Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors.
AID240338Effective concentration required for the activation of human K125A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165083Compound was measured for the antagonism of the activation of phospholipase C in mutant(S317A) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID242669Inhibition concentration required against human Y203F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID462462Induction of calcium flux in human 1321N1 cells at 10 uM by FLIPR assay2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Structure-activity relationship of (N)-Methanocarba phosphonate analogues of 5'-AMP as cardioprotective agents acting through a cardiac P2X receptor.
AID240349Effective concentration required for the activation of human R287K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID261696Activity against rat P2Y1-GFP transfected in HEK293 cells by intracellular calcium increase2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors.
AID240332Effective concentration required for the activation of human E209Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID150321Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2)2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Purine and pyrimidine (P2) receptors as drug targets.
AID150492Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 11; No effect as either agonist or antagonist at 10 uM2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.
AID373705Agonist activity at turkey P2Y1 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Identification of hydrolytically stable and selective P2Y(1) receptor agonists.
AID162984Relative half maximal velocity of Pyruvate kinase to Phosphoenolpyruvate was determined1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID242671Inhibition concentration required against human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240330Effective concentration required for the activation of human E209A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240355Effective concentration required for the activation of human S314T mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID242607Inhibition concentration required against wild type strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]-MRS2279 as radioligand2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID1415778Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using p-Nph-5'-TMP as substrate after 15 mins by capillary electrophoresis method2017MedChemComm, May-01, Volume: 8, Issue:5
Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors.
AID240347Effective concentration required for the activation of human R287A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165070Compound was measured for the antagonism of the activation of phospholipase C in mutant(H132A) human P2Y1 receptor in presence of MRS2179 (P<0.005)1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID165074Compound was measured for the antagonism of the activation of phospholipase C in mutant(K280A) human P2Y1 receptor in presence of MRS21791998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID165404Tested for relaxation of carbachol-contracted rabbit mesenteric artery at 37 degree C; Significantly more potent than 2MeSATP1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate.
AID1850681Displacement of [3H]-2MesADP from recombinant human P2Y12 transfected in HEK cell membrane assessed as inhibition constant2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Strategies for targeting the P2Y
AID165067Compound was measured for the antagonism of the activation of phospholipase C in mutant(F131A) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID240322Effective concentration required for the activation of human C202A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID227594Ratio of Km(ADP)/Ki or Km for rat kidney pyruvate kinase (PK-K)1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID240343Effective concentration required for the activation of human R128A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID240337Effective concentration required for the activation of human H277A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID1465394Selectivity ratio of EC50 for P2Y2 receptor Y306F mutant (unknown origin) to EC50 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
AID705929Agonist activity at turkey P2Y1R expressed in 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist.
AID1415777Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using ATP as substrate after 30 mins by capillary electrophoresis method2017MedChemComm, May-01, Volume: 8, Issue:5
Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors.
AID162991Michaelis-Menten constant for inhibition of pyruvate kinase obtained from rat muscle (PK-M) was determined using ADP as competitive inhibitor1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives.
AID165076Compound was measured for the antagonism of the activation of phospholipase C in mutant(Q307A) human P2Y1 receptor in presence of MRS21791998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID751213Agonist activity at human GFP-tagged P2Y1R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay2013Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12
Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists.
AID165077Compound was measured for the antagonism of the activation of phospholipase C in mutant(Q307A) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID240359Effective concentration required for the activation of human Y136A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID705926Metabolic stability in human serum assessed as hydrolysis of compound at 40 mM incubated for 24 hrs measured after every 1 hr over 24 hrs by HPLC2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist.
AID165069Compound was measured for the antagonism of the activation of phospholipase C in mutant(F226A) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID373709Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Identification of hydrolytically stable and selective P2Y(1) receptor agonists.
AID240356Effective concentration required for the activation of human S317A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID242672Inhibition concentration required against human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
AID165087Compound was measured for the antagonism of the activation of phospholipase C in mutant(T222A) human P2Y1 receptor.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
AID1346320Human P2Y12 receptor (P2Y receptors)2001Molecular pharmacology, Sep, Volume: 60, Issue:3
Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor.
AID1346309Human P2Y1 receptor (P2Y receptors)2001Molecular pharmacology, Sep, Volume: 60, Issue:3
Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor.
AID1346305Human P2Y13 receptor (P2Y receptors)2003Molecular pharmacology, Jul, Volume: 64, Issue:1
Pharmacological characterization of the human P2Y13 receptor.
AID1346309Human P2Y1 receptor (P2Y receptors)1997British journal of pharmacology, May, Volume: 121, Issue:2
An examination of deoxyadenosine 5'(alpha-thio)triphosphate as a ligand to define P2Y receptors and its selectivity as a low potency partial agonist of the P2Y1 receptor.
AID1346309Human P2Y1 receptor (P2Y receptors)2002Molecular pharmacology, Nov, Volume: 62, Issue:5
Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist.
AID1346320Human P2Y12 receptor (P2Y receptors)2003Seminars in vascular medicine, May, Volume: 3, Issue:2
P2Y12, a new platelet ADP receptor, target of clopidogrel.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (145)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906 (4.14)18.7374
1990's23 (15.86)18.2507
2000's60 (41.38)29.6817
2010's47 (32.41)24.3611
2020's9 (6.21)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.11

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index10.11 (24.57)
Research Supply Index5.00 (2.92)
Research Growth Index5.11 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (1.37%)5.53%
Reviews4 (2.74%)6.00%
Case Studies2 (1.37%)4.05%
Observational0 (0.00%)0.25%
Other138 (94.52%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]