Page last updated: 2024-08-05 15:26:20

purinergic receptor P2 antagonist

An antagonist at purinergic P2 receptors

ChEBI ID: 91079

Members (2)

MemberDefinitionClass
suraminA member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years.suramin
suramin sodiumAn organic sodium salt that is the hexasodium salt of suramin. It is an FDA approved drug for African sleeping sickness and river blindness.suramin sodium

Research

Studies (2,936)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990586 (19.96)18.7374
1990's1,112 (37.87)18.2507
2000's748 (25.48)29.6817
2010's406 (13.83)24.3611
2020's84 (2.86)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials92 (3.02%)5.53%
Reviews157 (5.16%)6.00%
Case Studies72 (2.37%)4.05%
Observational0 (0.00%)0.25%
Other2,722 (89.45%)84.16%

Protein Targets (103)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency7.079511
Bloom syndrome protein isoform 1Homo sapiens (human)Potency1.258911
caspase-1 isoform alpha precursorHomo sapiens (human)Potency39.810711
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.589311
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency23.587035
Chain A, Breast cancer type 1 susceptibility proteinHomo sapiens (human)Potency14.219112
Chain A, CruzipainTrypanosoma cruziPotency17.900812
Chain A, HADH2 proteinHomo sapiens (human)Potency12.533123
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency16.504335
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency4.921426
Chain B, HADH2 proteinHomo sapiens (human)Potency12.533123
DNA polymerase betaHomo sapiens (human)Potency0.891311
DNA polymerase eta isoform 1Homo sapiens (human)Potency0.223911
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency1.412511
DNA polymerase kappa isoform 1Homo sapiens (human)Potency0.065812
endonuclease IVEscherichia coliPotency9.296122
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency1.335712
EWS/FLI fusion proteinHomo sapiens (human)Potency10.476022
galactokinaseHomo sapiens (human)Potency17.782811
GLS proteinHomo sapiens (human)Potency8.912511
glucocerebrosidaseHomo sapiens (human)Potency22.387211
Glutamate receptor 1Rattus norvegicus (Norway rat)Potency8.912511
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency8.912511
Glutamate receptor 3Rattus norvegicus (Norway rat)Potency8.912511
Glutamate receptor 4Rattus norvegicus (Norway rat)Potency8.912511
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency3.162312
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency11.034412
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency12.589322
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency3.162311
Integrin alpha-IIbHomo sapiens (human)Potency12.589311
Integrin beta-3Homo sapiens (human)Potency12.589311
lamin isoform A-delta10Homo sapiens (human)Potency2.387722
LuciferasePhotinus pyralis (common eastern firefly)Potency27.536222
M-phase phosphoprotein 8Homo sapiens (human)Potency8.912511
Microtubule-associated protein tauHomo sapiens (human)Potency23.182226
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency1.584911
NFKB1 protein, partialHomo sapiens (human)Potency0.354822
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency31.622811
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency36.125411
phosphopantetheinyl transferaseBacillus subtilisPotency54.538812
Platelet-activating factor receptorHomo sapiens (human)Potency14.219112
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency3.162311
pyruvate kinaseLeishmania mexicana mexicanaPotency0.794322
pyruvate kinase PKM isoform bHomo sapiens (human)Potency31.622822
regulator of G-protein signaling 4Homo sapiens (human)Potency0.007511
survival motor neuron protein isoform dHomo sapiens (human)Potency11.220211
TDP1 proteinHomo sapiens (human)Potency6.513111
thioredoxin reductaseRattus norvegicus (Norway rat)Potency9.466211
ThrombopoietinHomo sapiens (human)Potency3.981122
thyroid stimulating hormone receptorHomo sapiens (human)Potency6.309622
USP1 protein, partialHomo sapiens (human)Potency7.943311
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency35.481311

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-dependent 6-phosphofructokinaseTrypanosoma brucei bruceiIC503.000011
Cathepsin BHomo sapiens (human)IC5030.000011
D(3) dopamine receptorRattus norvegicus (Norway rat)IC5018.100011
DNA primaseMycobacterium tuberculosis CDC1551IC508.200011
DNA-dependent protein kinase catalytic subunitHomo sapiens (human)IC501.700011
Dual specificity protein phosphatase 5Homo sapiens (human)Ki0.025011
Ectonucleoside triphosphate diphosphohydrolase 1Rattus norvegicus (Norway rat)Ki300.000022
Ectonucleoside triphosphate diphosphohydrolase 2Rattus norvegicus (Norway rat)Ki65.400022
Ectonucleoside triphosphate diphosphohydrolase 3 Rattus norvegicus (Norway rat)Ki12.700011
Ectonucleoside triphosphate diphosphohydrolase 8Homo sapiens (human)Ki100.000011
NAD-dependent protein deacetylase HST2Saccharomyces cerevisiae S288CIC50240.000011
NAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)IC501.385777
NAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)IC501.175044
NAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)IC5020.600088
P2X purinoceptor 2Rattus norvegicus (Norway rat)IC5021.905412
P2Y purinoceptor 11Homo sapiens (human)Ki0.207122
P2Y purinoceptor 2Homo sapiens (human)IC5075.000022
P2Y purinoceptor 6Homo sapiens (human)IC5027.000011
Protein arginine N-methyltransferase 1Homo sapiens (human)IC50344.810033
Protein kinase C alpha typeHomo sapiens (human)IC5029.000011
Protein kinase C beta typeHomo sapiens (human)IC5029.000011
Protein kinase C delta typeHomo sapiens (human)IC5029.000011
Protein kinase C epsilon typeHomo sapiens (human)IC5029.000011
Protein kinase C eta typeHomo sapiens (human)IC5029.000011
Protein kinase C gamma typeHomo sapiens (human)IC5029.000011
Protein kinase C iota typeHomo sapiens (human)IC5029.000011
Protein kinase C theta typeHomo sapiens (human)IC5029.000011
Protein kinase C zeta typeHomo sapiens (human)IC5029.000011
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC5012.200022
RmtAAspergillus nidulansIC505.900011
Serine/threonine-protein kinase D1Homo sapiens (human)IC5029.000011
Serine/threonine-protein kinase D3Homo sapiens (human)IC5029.000011
Signal transducer and activator of transcription 1-alpha/betaHomo sapiens (human)IC509.100011
Signal transducer and activator of transcription 3 Mus musculus (house mouse)IC50100.000011
Signal transducer and activator of transcription 5AHomo sapiens (human)IC509.400011
Signal transducer and activator of transcription 5BHomo sapiens (human)IC5010.400011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC509.760011
Uracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)IC50100.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Delta-type opioid receptorHomo sapiens (human)EC50100.000011
Kappa-type opioid receptorHomo sapiens (human)EC50100.000011
Mu-type opioid receptorHomo sapiens (human)EC50100.000011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC501.300011
P2X purinoceptor 1Rattus norvegicus (Norway rat)EC501.000011
P2X purinoceptor 2Rattus norvegicus (Norway rat)EC5010.400011
P2X purinoceptor 3Homo sapiens (human)EC508.950022
P2X purinoceptor 4Rattus norvegicus (Norway rat)EC50100.000011
P2X purinoceptor 5Rattus norvegicus (Norway rat)EC504.000011
P2X purinoceptor 6Rattus norvegicus (Norway rat)EC50100.000011
P2X purinoceptor 7Homo sapiens (human)EC5092.000011
P2Y purinoceptor 1Meleagris gallopavo (turkey)EC5010.000011
P2Y purinoceptor 11Homo sapiens (human)EC5016.000011
P2Y purinoceptor 12Rattus norvegicus (Norway rat)EC504.000011
P2Y purinoceptor 2Homo sapiens (human)EC5048.000011
P2Y purinoceptor 4Homo sapiens (human)EC50100.000011