Page last updated: 2024-11-12

af 353

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

Description

5-(5-iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine: a P2X3 and P2X2/3 receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID15953802
CHEMBL ID526307
SCHEMBL ID1494138
MeSH IDM0550868

Synonyms (31)

Synonym
5-(5-iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine
bdbm50257636
CHEMBL526307 ,
865305-30-2
A841708
5-(5-iodo-2-isopropyl-4-methoxy-phenoxy)pyrimidine-2,4-diamine;af-353
2,4-pyrimidinediamine, 5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-
gtpl4125
af 353
af353
af-353
5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidine-2,4-diamine
5-(5-iodo-2-isopropyl-4-methoxy-phenoxy) -pyrimidine-2,4-diamine
AATPYXMXFBBKFO-UHFFFAOYSA-N ,
5-(5-iodo-2-isopropyl-4-methoxy-phenoxy)-pyrimidine-2,4-diamine
CS-5061
SCHEMBL1494138
HY-14483
5-[5-iodo-4-methoxy-2-(propan-2-yl)phenoxy]pyrimidine-2,4-diamine
DTXSID90580447
AKOS026750345
ro-4
NCGC00484064-01
af-353(ro-4)
EX-A1635
Q27074324
BCP28391
AMY41794
MS-26787
S0405
BA165790

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Favourable pharmacokinetic parameters were observed in rat, with good oral bioavailability (%F = 32."( AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist.
Burnstock, G; Dillon, MP; Ford, AP; Gever, JR; Hackos, DH; Henningsen, RA; Martin, RS; Milla, ME; Oglesby, IB; Panicker, S; Rubas, W; Soto, R, 2010
)
0.36
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (11)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H2 receptorHomo sapiens (human)Ki100,000.00000.00062.197310.0000AID417920
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki100,000.00000.00000.385510.0000AID417921
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki100,000.00000.00000.74119.9000AID417922
P2X purinoceptor 3Rattus norvegicus (Norway rat)IC50 (µMol)0.01100.01000.08260.2400AID414332; AID417912
P2X purinoceptor 3Rattus norvegicus (Norway rat)Ki0.00980.00980.04030.0708AID1259561
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki100,000.00000.00020.522910.0000AID417923
P2X purinoceptor 1Homo sapiens (human)IC50 (µMol)10.00000.01922.346410.0000AID417914
P2X purinoceptor 3Homo sapiens (human)IC50 (µMol)0.04110.00000.20301.5136AID1627253; AID414333; AID417913
P2X purinoceptor 3Homo sapiens (human)Ki0.04170.00900.04660.0891AID1259562
P2X purinoceptor 5Homo sapiens (human)IC50 (µMol)10.00008.45008.45008.4500AID417917
P2X purinoceptor 4Homo sapiens (human)IC50 (µMol)10.00000.15602.93526.1000AID417916
P2X purinoceptor 7Homo sapiens (human)IC50 (µMol)10.00000.00080.24525.0000AID417918
P2X purinoceptor 2Homo sapiens (human)IC50 (µMol)2.53610.00830.43452.0200AID414333; AID417913; AID417915
P2X purinoceptor 2Homo sapiens (human)Ki0.04170.00900.04660.0891AID1259562
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (170)

Processvia Protein(s)Taxonomy
gastric acid secretionHistamine H2 receptorHomo sapiens (human)
immune responseHistamine H2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H2 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H2 receptorHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
monoatomic ion transportP2X purinoceptor 1Homo sapiens (human)
serotonin secretion by plateletP2X purinoceptor 1Homo sapiens (human)
regulation of vascular associated smooth muscle contractionP2X purinoceptor 1Homo sapiens (human)
apoptotic processP2X purinoceptor 1Homo sapiens (human)
signal transductionP2X purinoceptor 1Homo sapiens (human)
inseminationP2X purinoceptor 1Homo sapiens (human)
regulation of blood pressureP2X purinoceptor 1Homo sapiens (human)
neuronal action potentialP2X purinoceptor 1Homo sapiens (human)
calcium-mediated signalingP2X purinoceptor 1Homo sapiens (human)
platelet activationP2X purinoceptor 1Homo sapiens (human)
response to ATPP2X purinoceptor 1Homo sapiens (human)
synaptic transmission, glutamatergicP2X purinoceptor 1Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 1Homo sapiens (human)
ceramide biosynthetic processP2X purinoceptor 1Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationP2X purinoceptor 1Homo sapiens (human)
positive regulation of calcium ion import across plasma membraneP2X purinoceptor 1Homo sapiens (human)
regulation of synaptic vesicle exocytosisP2X purinoceptor 1Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 1Homo sapiens (human)
response to hypoxiaP2X purinoceptor 3Homo sapiens (human)
signal transductionP2X purinoceptor 3Homo sapiens (human)
neuromuscular synaptic transmissionP2X purinoceptor 3Homo sapiens (human)
response to heatP2X purinoceptor 3Homo sapiens (human)
response to coldP2X purinoceptor 3Homo sapiens (human)
response to mechanical stimulusP2X purinoceptor 3Homo sapiens (human)
response to carbohydrateP2X purinoceptor 3Homo sapiens (human)
positive regulation of calcium ion transport into cytosolP2X purinoceptor 3Homo sapiens (human)
urinary bladder smooth muscle contractionP2X purinoceptor 3Homo sapiens (human)
peristalsisP2X purinoceptor 3Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 3Homo sapiens (human)
regulation of synaptic plasticityP2X purinoceptor 3Homo sapiens (human)
behavioral response to painP2X purinoceptor 3Homo sapiens (human)
positive regulation of calcium-mediated signalingP2X purinoceptor 3Homo sapiens (human)
sensory perception of tasteP2X purinoceptor 3Homo sapiens (human)
establishment of localization in cellP2X purinoceptor 3Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 3Homo sapiens (human)
protein homotrimerizationP2X purinoceptor 3Homo sapiens (human)
cellular response to ATPP2X purinoceptor 3Homo sapiens (human)
inorganic cation transmembrane transportP2X purinoceptor 3Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 3Homo sapiens (human)
chloride transportP2X purinoceptor 5Homo sapiens (human)
signal transductionP2X purinoceptor 5Homo sapiens (human)
nervous system developmentP2X purinoceptor 5Homo sapiens (human)
positive regulation of calcium ion transport into cytosolP2X purinoceptor 5Homo sapiens (human)
response to ATPP2X purinoceptor 5Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 5Homo sapiens (human)
osteoclast maturationP2X purinoceptor 5Homo sapiens (human)
positive regulation of calcium-mediated signalingP2X purinoceptor 5Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 5Homo sapiens (human)
monoatomic anion transmembrane transportP2X purinoceptor 5Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 5Homo sapiens (human)
regulation of ruffle assemblyP2X purinoceptor 4Homo sapiens (human)
tissue homeostasisP2X purinoceptor 4Homo sapiens (human)
regulation of sodium ion transportP2X purinoceptor 4Homo sapiens (human)
response to ischemiaP2X purinoceptor 4Homo sapiens (human)
signal transductionP2X purinoceptor 4Homo sapiens (human)
regulation of blood pressureP2X purinoceptor 4Homo sapiens (human)
positive regulation of calcium ion transport into cytosolP2X purinoceptor 4Homo sapiens (human)
negative regulation of cardiac muscle hypertrophyP2X purinoceptor 4Homo sapiens (human)
neuronal action potentialP2X purinoceptor 4Homo sapiens (human)
sensory perception of painP2X purinoceptor 4Homo sapiens (human)
calcium-mediated signalingP2X purinoceptor 4Homo sapiens (human)
positive regulation of prostaglandin secretionP2X purinoceptor 4Homo sapiens (human)
response to ATPP2X purinoceptor 4Homo sapiens (human)
monoatomic ion transmembrane transportP2X purinoceptor 4Homo sapiens (human)
response to fluid shear stressP2X purinoceptor 4Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 4Homo sapiens (human)
endothelial cell activationP2X purinoceptor 4Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationP2X purinoceptor 4Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processP2X purinoceptor 4Homo sapiens (human)
behavioral response to painP2X purinoceptor 4Homo sapiens (human)
response to axon injuryP2X purinoceptor 4Homo sapiens (human)
positive regulation of calcium-mediated signalingP2X purinoceptor 4Homo sapiens (human)
regulation of chemotaxisP2X purinoceptor 4Homo sapiens (human)
sensory perception of touchP2X purinoceptor 4Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionP2X purinoceptor 4Homo sapiens (human)
membrane depolarizationP2X purinoceptor 4Homo sapiens (human)
positive regulation of calcium ion transportP2X purinoceptor 4Homo sapiens (human)
regulation of cardiac muscle contractionP2X purinoceptor 4Homo sapiens (human)
relaxation of cardiac muscleP2X purinoceptor 4Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 4Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 4Homo sapiens (human)
cellular response to zinc ionP2X purinoceptor 4Homo sapiens (human)
cellular response to ATPP2X purinoceptor 4Homo sapiens (human)
apoptotic signaling pathwayP2X purinoceptor 4Homo sapiens (human)
positive regulation of microglial cell migrationP2X purinoceptor 4Homo sapiens (human)
positive regulation of endothelial cell chemotaxisP2X purinoceptor 4Homo sapiens (human)
MAPK cascadeP2X purinoceptor 7Homo sapiens (human)
cell morphogenesisP2X purinoceptor 7Homo sapiens (human)
phagolysosome assemblyP2X purinoceptor 7Homo sapiens (human)
T cell mediated cytotoxicityP2X purinoceptor 7Homo sapiens (human)
positive regulation of T cell mediated cytotoxicityP2X purinoceptor 7Homo sapiens (human)
positive regulation of protein phosphorylationP2X purinoceptor 7Homo sapiens (human)
regulation of sodium ion transportP2X purinoceptor 7Homo sapiens (human)
response to ischemiaP2X purinoceptor 7Homo sapiens (human)
membrane protein ectodomain proteolysisP2X purinoceptor 7Homo sapiens (human)
phospholipid transfer to membraneP2X purinoceptor 7Homo sapiens (human)
vesicle budding from membraneP2X purinoceptor 7Homo sapiens (human)
inflammatory responseP2X purinoceptor 7Homo sapiens (human)
mitochondrion organizationP2X purinoceptor 7Homo sapiens (human)
cell surface receptor signaling pathwayP2X purinoceptor 7Homo sapiens (human)
protein secretionP2X purinoceptor 7Homo sapiens (human)
response to xenobiotic stimulusP2X purinoceptor 7Homo sapiens (human)
response to mechanical stimulusP2X purinoceptor 7Homo sapiens (human)
response to zinc ionP2X purinoceptor 7Homo sapiens (human)
positive regulation of calcium ion transport into cytosolP2X purinoceptor 7Homo sapiens (human)
positive regulation of gene expressionP2X purinoceptor 7Homo sapiens (human)
glutamate secretionP2X purinoceptor 7Homo sapiens (human)
positive regulation of glutamate secretionP2X purinoceptor 7Homo sapiens (human)
gamma-aminobutyric acid secretionP2X purinoceptor 7Homo sapiens (human)
positive regulation of gamma-aminobutyric acid secretionP2X purinoceptor 7Homo sapiens (human)
synaptic vesicle exocytosisP2X purinoceptor 7Homo sapiens (human)
protein processingP2X purinoceptor 7Homo sapiens (human)
plasma membrane phospholipid scramblingP2X purinoceptor 7Homo sapiens (human)
sensory perception of painP2X purinoceptor 7Homo sapiens (human)
calcium-mediated signalingP2X purinoceptor 7Homo sapiens (human)
protein catabolic processP2X purinoceptor 7Homo sapiens (human)
positive regulation of bone mineralizationP2X purinoceptor 7Homo sapiens (human)
bleb assemblyP2X purinoceptor 7Homo sapiens (human)
positive regulation of prostaglandin secretionP2X purinoceptor 7Homo sapiens (human)
prostaglandin secretionP2X purinoceptor 7Homo sapiens (human)
response to lipopolysaccharideP2X purinoceptor 7Homo sapiens (human)
positive regulation of interleukin-1 alpha productionP2X purinoceptor 7Homo sapiens (human)
positive regulation of interleukin-1 beta productionP2X purinoceptor 7Homo sapiens (human)
positive regulation of interleukin-6 productionP2X purinoceptor 7Homo sapiens (human)
collagen metabolic processP2X purinoceptor 7Homo sapiens (human)
response to ATPP2X purinoceptor 7Homo sapiens (human)
response to fluid shear stressP2X purinoceptor 7Homo sapiens (human)
positive regulation of monoatomic ion transmembrane transportP2X purinoceptor 7Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 7Homo sapiens (human)
T cell proliferationP2X purinoceptor 7Homo sapiens (human)
T cell homeostasisP2X purinoceptor 7Homo sapiens (human)
NAD transportP2X purinoceptor 7Homo sapiens (human)
negative regulation of MAPK cascadeP2X purinoceptor 7Homo sapiens (human)
positive regulation of MAPK cascadeP2X purinoceptor 7Homo sapiens (human)
negative regulation of bone resorptionP2X purinoceptor 7Homo sapiens (human)
negative regulation of cell volumeP2X purinoceptor 7Homo sapiens (human)
positive regulation of glycolytic processP2X purinoceptor 7Homo sapiens (human)
ceramide biosynthetic processP2X purinoceptor 7Homo sapiens (human)
pore complex assemblyP2X purinoceptor 7Homo sapiens (human)
skeletal system morphogenesisP2X purinoceptor 7Homo sapiens (human)
homeostasis of number of cells within a tissueP2X purinoceptor 7Homo sapiens (human)
positive regulation of protein secretionP2X purinoceptor 7Homo sapiens (human)
defense response to Gram-positive bacteriumP2X purinoceptor 7Homo sapiens (human)
release of sequestered calcium ion into cytosolP2X purinoceptor 7Homo sapiens (human)
positive regulation of cytoskeleton organizationP2X purinoceptor 7Homo sapiens (human)
response to calcium ionP2X purinoceptor 7Homo sapiens (human)
response to electrical stimulusP2X purinoceptor 7Homo sapiens (human)
mitochondrial depolarizationP2X purinoceptor 7Homo sapiens (human)
membrane depolarizationP2X purinoceptor 7Homo sapiens (human)
positive regulation of mitochondrial depolarizationP2X purinoceptor 7Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 7Homo sapiens (human)
positive regulation of macrophage cytokine productionP2X purinoceptor 7Homo sapiens (human)
T cell apoptotic processP2X purinoceptor 7Homo sapiens (human)
positive regulation of T cell apoptotic processP2X purinoceptor 7Homo sapiens (human)
cellular response to ATPP2X purinoceptor 7Homo sapiens (human)
cellular response to dsRNAP2X purinoceptor 7Homo sapiens (human)
reactive oxygen species metabolic processP2X purinoceptor 7Homo sapiens (human)
apoptotic signaling pathwayP2X purinoceptor 7Homo sapiens (human)
extrinsic apoptotic signaling pathwayP2X purinoceptor 7Homo sapiens (human)
positive regulation of bleb assemblyP2X purinoceptor 7Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 7Homo sapiens (human)
response to hypoxiaP2X purinoceptor 2Homo sapiens (human)
response to ischemiaP2X purinoceptor 2Homo sapiens (human)
detection of hypoxic conditions in blood by carotid body chemoreceptor signalingP2X purinoceptor 2Homo sapiens (human)
neuromuscular synaptic transmissionP2X purinoceptor 2Homo sapiens (human)
neuromuscular junction developmentP2X purinoceptor 2Homo sapiens (human)
sensory perception of soundP2X purinoceptor 2Homo sapiens (human)
response to carbohydrateP2X purinoceptor 2Homo sapiens (human)
positive regulation of calcium ion transport into cytosolP2X purinoceptor 2Homo sapiens (human)
urinary bladder smooth muscle contractionP2X purinoceptor 2Homo sapiens (human)
peristalsisP2X purinoceptor 2Homo sapiens (human)
response to ATPP2X purinoceptor 2Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 2Homo sapiens (human)
behavioral response to painP2X purinoceptor 2Homo sapiens (human)
skeletal muscle fiber developmentP2X purinoceptor 2Homo sapiens (human)
positive regulation of calcium-mediated signalingP2X purinoceptor 2Homo sapiens (human)
sensory perception of tasteP2X purinoceptor 2Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 2Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (31)

Processvia Protein(s)Taxonomy
histamine receptor activityHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H2 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H2 receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
purinergic nucleotide receptor activityP2X purinoceptor 1Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 1Homo sapiens (human)
monoatomic cation channel activityP2X purinoceptor 1Homo sapiens (human)
protein bindingP2X purinoceptor 1Homo sapiens (human)
ATP bindingP2X purinoceptor 1Homo sapiens (human)
identical protein bindingP2X purinoceptor 1Homo sapiens (human)
suramin bindingP2X purinoceptor 1Homo sapiens (human)
protein-containing complex bindingP2X purinoceptor 1Homo sapiens (human)
ligand-gated calcium channel activityP2X purinoceptor 1Homo sapiens (human)
purinergic nucleotide receptor activityP2X purinoceptor 3Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 3Homo sapiens (human)
ATP bindingP2X purinoceptor 3Homo sapiens (human)
purinergic nucleotide receptor activityP2X purinoceptor 5Homo sapiens (human)
transmembrane signaling receptor activityP2X purinoceptor 5Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 5Homo sapiens (human)
monoatomic ion channel activityP2X purinoceptor 5Homo sapiens (human)
ATP bindingP2X purinoceptor 5Homo sapiens (human)
ATP-gated ion channel activityP2X purinoceptor 5Homo sapiens (human)
ligand-gated monoatomic anion channel activityP2X purinoceptor 5Homo sapiens (human)
purinergic nucleotide receptor activityP2X purinoceptor 4Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 4Homo sapiens (human)
signaling receptor bindingP2X purinoceptor 4Homo sapiens (human)
copper ion bindingP2X purinoceptor 4Homo sapiens (human)
protein bindingP2X purinoceptor 4Homo sapiens (human)
ATP bindingP2X purinoceptor 4Homo sapiens (human)
zinc ion bindingP2X purinoceptor 4Homo sapiens (human)
identical protein bindingP2X purinoceptor 4Homo sapiens (human)
cadherin bindingP2X purinoceptor 4Homo sapiens (human)
ligand-gated calcium channel activityP2X purinoceptor 4Homo sapiens (human)
lipopolysaccharide bindingP2X purinoceptor 7Homo sapiens (human)
purinergic nucleotide receptor activityP2X purinoceptor 7Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 7Homo sapiens (human)
signaling receptor bindingP2X purinoceptor 7Homo sapiens (human)
protein bindingP2X purinoceptor 7Homo sapiens (human)
ATP bindingP2X purinoceptor 7Homo sapiens (human)
identical protein bindingP2X purinoceptor 7Homo sapiens (human)
purinergic nucleotide receptor activityP2X purinoceptor 2Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 2Homo sapiens (human)
ATP bindingP2X purinoceptor 2Homo sapiens (human)
ligand-gated monoatomic ion channel activityP2X purinoceptor 2Homo sapiens (human)
identical protein bindingP2X purinoceptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (46)

Processvia Protein(s)Taxonomy
plasma membraneHistamine H2 receptorHomo sapiens (human)
synapseHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
dendriteHistamine H2 receptorHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membraneP2X purinoceptor 1Homo sapiens (human)
external side of plasma membraneP2X purinoceptor 1Homo sapiens (human)
secretory granule membraneP2X purinoceptor 1Homo sapiens (human)
specific granule membraneP2X purinoceptor 1Homo sapiens (human)
membrane raftP2X purinoceptor 1Homo sapiens (human)
postsynaptic membraneP2X purinoceptor 1Homo sapiens (human)
presynaptic active zone membraneP2X purinoceptor 1Homo sapiens (human)
glutamatergic synapseP2X purinoceptor 1Homo sapiens (human)
protein-containing complexP2X purinoceptor 1Homo sapiens (human)
plasma membraneP2X purinoceptor 1Homo sapiens (human)
plasma membraneP2X purinoceptor 3Homo sapiens (human)
axonP2X purinoceptor 3Homo sapiens (human)
Schaffer collateral - CA1 synapseP2X purinoceptor 3Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseP2X purinoceptor 3Homo sapiens (human)
postsynapseP2X purinoceptor 3Homo sapiens (human)
receptor complexP2X purinoceptor 3Homo sapiens (human)
plasma membraneP2X purinoceptor 3Homo sapiens (human)
cytosolP2X purinoceptor 5Homo sapiens (human)
plasma membraneP2X purinoceptor 5Homo sapiens (human)
postsynapseP2X purinoceptor 5Homo sapiens (human)
plasma membraneP2X purinoceptor 5Homo sapiens (human)
lysosomal membraneP2X purinoceptor 4Homo sapiens (human)
plasma membraneP2X purinoceptor 4Homo sapiens (human)
membraneP2X purinoceptor 4Homo sapiens (human)
cell junctionP2X purinoceptor 4Homo sapiens (human)
neuronal cell bodyP2X purinoceptor 4Homo sapiens (human)
terminal boutonP2X purinoceptor 4Homo sapiens (human)
dendritic spineP2X purinoceptor 4Homo sapiens (human)
cell bodyP2X purinoceptor 4Homo sapiens (human)
perinuclear region of cytoplasmP2X purinoceptor 4Homo sapiens (human)
extracellular exosomeP2X purinoceptor 4Homo sapiens (human)
plasma membraneP2X purinoceptor 4Homo sapiens (human)
cytoplasmP2X purinoceptor 7Homo sapiens (human)
mitochondrionP2X purinoceptor 7Homo sapiens (human)
plasma membraneP2X purinoceptor 7Homo sapiens (human)
cell-cell junctionP2X purinoceptor 7Homo sapiens (human)
external side of plasma membraneP2X purinoceptor 7Homo sapiens (human)
membraneP2X purinoceptor 7Homo sapiens (human)
neuromuscular junctionP2X purinoceptor 7Homo sapiens (human)
blebP2X purinoceptor 7Homo sapiens (human)
neuronal cell bodyP2X purinoceptor 7Homo sapiens (human)
presynapseP2X purinoceptor 7Homo sapiens (human)
postsynapseP2X purinoceptor 7Homo sapiens (human)
plasma membraneP2X purinoceptor 7Homo sapiens (human)
plasma membraneP2X purinoceptor 2Homo sapiens (human)
apical plasma membraneP2X purinoceptor 2Homo sapiens (human)
neuronal cell bodyP2X purinoceptor 2Homo sapiens (human)
postsynapseP2X purinoceptor 2Homo sapiens (human)
neuronal dense core vesicleP2X purinoceptor 2Homo sapiens (human)
receptor complexP2X purinoceptor 2Homo sapiens (human)
plasma membraneP2X purinoceptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (43)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID417925Oral bioavailability in dog2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414350Clearance in dog2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414332Antagonist activity at rat P2X3 receptor expressed in CHO cells by FLIPR2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414341Tmax in rat at 2 mg/kg, po administered as single dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414345AUC in rat at 2 mg/kg, po administered as single dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417923Inhibition of 5HT6 receptor2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414333Antagonist activity at human P2X2/3 receptor expressed in 1321n1c cells by FLIPR2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414349Oral bioavailability in rat at 2 mg/kg administered as single dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417912Antagonist activity at rat recombinant P2X3 receptor expressed in CHO cells by FLIPR assay2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414340Tmax in rat at 2 mg/kg, iv administered as single dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417917Inhibition of P2X5 receptor2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417926Half life in dog2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417920Inhibition of histamine H2 receptor2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414344AUC in rat at 2 mg/kg, iv administered as single dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417921Inhibition of 5HT2A receptor2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414348Clearance in rat at 2 mg/kg, iv administered as single dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417911Oral bioavailability in dog2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417919Inhibition of ML1 receptor2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID1627256Intrinsic clearance in human liver microsomes at 1 to 2.5 uM in presence of NADPH2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds.
AID1627258Ratio of efflux to influx in human Caco2 cells2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds.
AID417918Inhibition of P2X7 receptor2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID1627253Antagonist activity at human recombinant P2X3 receptor expressed in HEK293-Tet-on cells assessed as alpha,beta-methylene-ATP-stimulated Ca2+ influx by Fluo-4 assay2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds.
AID417922Inhibition of 5HT3 receptor2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID1627257Permeability in vinblastine-treated human Caco2 cells2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds.
AID414586Half life in dog2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417914Inhibition of P2X1 receptor2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417913Antagonist activity at human recombinant P2X2/3 receptor expressed in human 1321N1 cells by FLIPR assay2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414347Half life in rat at 2 mg/kg, po administered as single dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID1627255Kinetic solubility of the compound in phosphate buffer at pH 7.4 by HPLC analysis2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds.
AID417915Inhibition of P2X2 receptor2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417916Inhibition of P2X4 receptor2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417927Ratio of permeability from basolateral to apical side over apical to basolateral side in human Caco-2 cells2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID1627259Inhibition of human ERG relative to control2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds.
AID414343Cmax in rat at 2 mg/kg, po administered as single dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414342Cmax in rat at 2 mg/kg, iv administered as single dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417924Clearance in dog2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID414346Half life in rat at 2 mg/kg, iv administered as single dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID1346621Human P2X3 (P2X receptors)2010British journal of pharmacology, Jul, Volume: 160, Issue:6
AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (16.67)29.6817
2010's6 (50.00)24.3611
2020's4 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.62

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 Index29.62 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.87 (4.65)
Search Engine Demand Index59.35 (26.88)
Search Engine Supply Index3.76 (0.95)

This Compound (29.62)

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%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]