Page last updated: 2024-12-10

mrs2159

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Description

MRS2159: an antagonist of both P2X1 and P2X7 receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5052387
CHEMBL ID119235
CHEMBL ID1617474
SCHEMBL ID14702229
SCHEMBL ID21033370
MeSH IDM000611322

Synonyms (18)

Synonym
LOPAC0_000780
mrs2159
CHEMBL119235 ,
bdbm50102295
4-(4-formyl-5-hydroxy-6-methyl-3-phosphonooxymethyl-pyridin-2-ylazo)-benzoic acid
4-[(e)-{4-formyl-5-hydroxy-6-methyl-3-[(phosphonooxy)methyl]pyridin-2-yl}diazenyl]benzoic acid
fobisin101
SCHEMBL14702229
CHEMBL1617474
SCHEMBL21033370
219554-18-4
mrs-2159
CCG-208810
gtpl11231
4-[[4-formyl-5-hydroxy-6-methyl-3-(phosphonooxymethyl)pyridin-2-yl]diazenyl]benzoic acid
DTXSID601017383
4-[(4-formyl-5hydroxy-6-methyl-3-[(phosphonooxy)methyl}-2-pyridinyl)azo]benzoic acid
Q27454060
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
P2X purinoceptor 1Rattus norvegicus (Norway rat)IC50 (µMol)0.02620.00030.23031.0000AID1059220; AID150300
P2Y purinoceptor 1Meleagris gallopavo (turkey)IC50 (µMol)100.00004.19006.04258.4600AID150644
P2X purinoceptor 2Rattus norvegicus (Norway rat)IC50 (µMol)11.90000.69001.65804.0000AID150303
P2X purinoceptor 3Rattus norvegicus (Norway rat)IC50 (µMol)0.14000.01000.08260.2400AID150305
P2X purinoceptor 1Mus musculus (house mouse)IC50 (µMol)0.03000.03000.06450.0990AID1059228
14-3-3 protein zeta/deltaHomo sapiens (human)IC50 (µMol)9.30009.30009.30009.3000AID1393200; AID1473395
P2X purinoceptor 7Homo sapiens (human)IC50 (µMol)0.60000.00080.24525.0000AID744381
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (101)

Processvia Protein(s)Taxonomy
negative regulation of protein kinase activity14-3-3 protein gammaHomo sapiens (human)
protein targeting14-3-3 protein gammaHomo sapiens (human)
regulation of signal transduction14-3-3 protein gammaHomo sapiens (human)
cellular response to insulin stimulus14-3-3 protein gammaHomo sapiens (human)
cellular response to glucose starvation14-3-3 protein gammaHomo sapiens (human)
regulation of neuron differentiation14-3-3 protein gammaHomo sapiens (human)
regulation of synaptic plasticity14-3-3 protein gammaHomo sapiens (human)
negative regulation of TORC1 signaling14-3-3 protein gammaHomo sapiens (human)
signal transduction14-3-3 protein gammaHomo sapiens (human)
protein localization14-3-3 protein gammaHomo sapiens (human)
negative regulation of transcription by RNA polymerase II14-3-3 protein zeta/deltaHomo sapiens (human)
angiogenesis14-3-3 protein zeta/deltaHomo sapiens (human)
respiratory system process14-3-3 protein zeta/deltaHomo sapiens (human)
protein phosphorylation14-3-3 protein zeta/deltaHomo sapiens (human)
protein targeting14-3-3 protein zeta/deltaHomo sapiens (human)
signal transduction14-3-3 protein zeta/deltaHomo sapiens (human)
synaptic target recognition14-3-3 protein zeta/deltaHomo sapiens (human)
lung development14-3-3 protein zeta/deltaHomo sapiens (human)
regulation of protein stability14-3-3 protein zeta/deltaHomo sapiens (human)
tube formation14-3-3 protein zeta/deltaHomo sapiens (human)
cellular response to glucose starvation14-3-3 protein zeta/deltaHomo sapiens (human)
negative regulation of apoptotic process14-3-3 protein zeta/deltaHomo sapiens (human)
negative regulation of innate immune response14-3-3 protein zeta/deltaHomo sapiens (human)
establishment of Golgi localization14-3-3 protein zeta/deltaHomo sapiens (human)
ERK1 and ERK2 cascade14-3-3 protein zeta/deltaHomo sapiens (human)
regulation of ERK1 and ERK2 cascade14-3-3 protein zeta/deltaHomo sapiens (human)
regulation of synapse maturation14-3-3 protein zeta/deltaHomo sapiens (human)
Golgi reassembly14-3-3 protein zeta/deltaHomo sapiens (human)
negative regulation of protein localization to nucleus14-3-3 protein zeta/deltaHomo sapiens (human)
negative regulation of TORC1 signaling14-3-3 protein zeta/deltaHomo sapiens (human)
protein localization14-3-3 protein zeta/deltaHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
RNA binding14-3-3 protein gammaHomo sapiens (human)
protein kinase C binding14-3-3 protein gammaHomo sapiens (human)
insulin-like growth factor receptor binding14-3-3 protein gammaHomo sapiens (human)
protein binding14-3-3 protein gammaHomo sapiens (human)
protein kinase C inhibitor activity14-3-3 protein gammaHomo sapiens (human)
protein domain specific binding14-3-3 protein gammaHomo sapiens (human)
receptor tyrosine kinase binding14-3-3 protein gammaHomo sapiens (human)
identical protein binding14-3-3 protein gammaHomo sapiens (human)
phosphorylation-dependent protein binding14-3-3 protein gammaHomo sapiens (human)
protein sequestering activity14-3-3 protein gammaHomo sapiens (human)
RNA binding14-3-3 protein zeta/deltaHomo sapiens (human)
protein binding14-3-3 protein zeta/deltaHomo sapiens (human)
protein kinase binding14-3-3 protein zeta/deltaHomo sapiens (human)
protein domain specific binding14-3-3 protein zeta/deltaHomo sapiens (human)
ubiquitin protein ligase binding14-3-3 protein zeta/deltaHomo sapiens (human)
identical protein binding14-3-3 protein zeta/deltaHomo sapiens (human)
transmembrane transporter binding14-3-3 protein zeta/deltaHomo sapiens (human)
cadherin binding14-3-3 protein zeta/deltaHomo sapiens (human)
phosphoserine residue binding14-3-3 protein zeta/deltaHomo sapiens (human)
DNA-binding transcription factor binding14-3-3 protein zeta/deltaHomo sapiens (human)
protein sequestering activity14-3-3 protein zeta/deltaHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
cytosol14-3-3 protein gammaHomo sapiens (human)
focal adhesion14-3-3 protein gammaHomo sapiens (human)
membrane14-3-3 protein gammaHomo sapiens (human)
extracellular exosome14-3-3 protein gammaHomo sapiens (human)
presynapse14-3-3 protein gammaHomo sapiens (human)
cytoplasm14-3-3 protein gammaHomo sapiens (human)
cytosol14-3-3 protein zeta/deltaHomo sapiens (human)
glutamatergic synapse14-3-3 protein zeta/deltaHomo sapiens (human)
extracellular space14-3-3 protein zeta/deltaHomo sapiens (human)
nucleus14-3-3 protein zeta/deltaHomo sapiens (human)
nucleoplasm14-3-3 protein zeta/deltaHomo sapiens (human)
cytosol14-3-3 protein zeta/deltaHomo sapiens (human)
focal adhesion14-3-3 protein zeta/deltaHomo sapiens (human)
vesicle14-3-3 protein zeta/deltaHomo sapiens (human)
melanosome14-3-3 protein zeta/deltaHomo sapiens (human)
extracellular exosome14-3-3 protein zeta/deltaHomo sapiens (human)
blood microparticle14-3-3 protein zeta/deltaHomo sapiens (human)
hippocampal mossy fiber to CA3 synapse14-3-3 protein zeta/deltaHomo sapiens (human)
cytoplasm14-3-3 protein zeta/deltaHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID1059228Antagonist activity at recombinant mouse P2X1 receptor expressed in Xenopus oocytes assessed as inhibition of ATP-induced ion current preincubated for 20 mins followed by ATP addition by two-electrode voltage clamp assay2013European journal of medicinal chemistry, , Volume: 70Design and synthesis of potent and selective P2X₃ receptor antagonists derived from PPADS as potential pain modulators.
AID1393201Binding affinity to GST-tagged 14-3-3-gamma (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibition of interaction with PRAS40 in African green monkey COS7 cells preincubated with protein followed by cell addition by ELISA2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Modulators of 14-3-3 Protein-Protein Interactions.
AID1473395Inhibition of PRAS40 binding to human GST-tagged 14-3-3 protein zeta/delta expressed in Escherichia coli BL21(DE3) by ELISA2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
X-ray Structures of Target-Ligand Complexes Containing Compounds with Assay Interference Potential.
AID150303Inhibition of inward ion current elicited by ATP at P2X2 receptor expressed in Xenopus oocytes2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors.
AID150644Inhibition of 10 nM 2-MeS-ADP-stimulated phospholipase C in turkey erythrocyte membranes using [3H]inositol2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors.
AID150305Inhibition of inward ion current elicited by ATP was determined at recombinant P2X3 receptor expressed in Xenopus oocytes2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors.
AID1059220Antagonist activity at recombinant rat P2X1 receptor expressed in Xenopus oocytes assessed as ion flux stimulation2013European journal of medicinal chemistry, , Volume: 70Design and synthesis of potent and selective P2X₃ receptor antagonists derived from PPADS as potential pain modulators.
AID744381Antagonist activity at P2X7 receptor (unknown origin)2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Synthesis and structure-activity relationships of carboxylic acid derivatives of pyridoxal as P2X receptor antagonists.
AID1393200Binding affinity to GST-tagged 14-3-3-zeta (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibition of interaction with PRAS40 in African green monkey COS7 cells preincubated with protein followed by cell addition by ELISA2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Modulators of 14-3-3 Protein-Protein Interactions.
AID150300Inhibition of inward ion current elicited by ATP at P2X1 receptor expressed in Xenopus oocytes2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (22.22)29.6817
2010's7 (77.78)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]