Page last updated: 2024-08-05 15:26:20
purinergic receptor P2 antagonist
An antagonist at purinergic P2 receptors
ChEBI ID: 91079
Members (2)
| Member | Definition | Class |
|---|---|---|
| suramin | A 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 sodium | An 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)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 586 (19.96) | 18.7374 |
| 1990's | 1,112 (37.87) | 18.2507 |
| 2000's | 748 (25.48) | 29.6817 |
| 2010's | 406 (13.83) | 24.3611 |
| 2020's | 84 (2.86) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 92 (3.02%) | 5.53% |
| Reviews | 157 (5.16%) | 6.00% |
| Case Studies | 72 (2.37%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 2,722 (89.45%) | 84.16% |
Protein Targets (103)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 7.0795 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 1.2589 | 1 | 1 |
| caspase-1 isoform alpha precursor | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 23.5870 | 3 | 5 |
| Chain A, Breast cancer type 1 susceptibility protein | Homo sapiens (human) | Potency | 14.2191 | 1 | 2 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 17.9008 | 1 | 2 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 12.5331 | 2 | 3 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 16.5043 | 3 | 5 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 4.9214 | 2 | 6 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 12.5331 | 2 | 3 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 0.8913 | 1 | 1 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 0.2239 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 1.4125 | 1 | 1 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 0.0658 | 1 | 2 |
| endonuclease IV | Escherichia coli | Potency | 9.2961 | 2 | 2 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 1.3357 | 1 | 2 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 10.4760 | 2 | 2 |
| galactokinase | Homo sapiens (human) | Potency | 17.7828 | 1 | 1 |
| GLS protein | Homo sapiens (human) | Potency | 8.9125 | 1 | 1 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | Potency | 8.9125 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 8.9125 | 1 | 1 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | Potency | 8.9125 | 1 | 1 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | Potency | 8.9125 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 3.1623 | 1 | 2 |
| histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 11.0344 | 1 | 2 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 2.3877 | 2 | 2 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 27.5362 | 2 | 2 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 8.9125 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 23.1822 | 2 | 6 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 0.3548 | 2 | 2 |
| Ornithine decarboxylase | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 36.1254 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 54.5388 | 1 | 2 |
| Platelet-activating factor receptor | Homo sapiens (human) | Potency | 14.2191 | 1 | 2 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| pyruvate kinase | Leishmania mexicana mexicana | Potency | 0.7943 | 2 | 2 |
| pyruvate kinase PKM isoform b | Homo sapiens (human) | Potency | 31.6228 | 2 | 2 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 0.0075 | 1 | 1 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 6.5131 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 9.4662 | 1 | 1 |
| Thrombopoietin | Homo sapiens (human) | Potency | 3.9811 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 6.3096 | 2 | 2 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 7.9433 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| ATP-dependent 6-phosphofructokinase | Trypanosoma brucei brucei | IC50 | 3.0000 | 1 | 1 |
| Cathepsin B | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| D(3) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 | 18.1000 | 1 | 1 |
| DNA primase | Mycobacterium tuberculosis CDC1551 | IC50 | 8.2000 | 1 | 1 |
| DNA-dependent protein kinase catalytic subunit | Homo sapiens (human) | IC50 | 1.7000 | 1 | 1 |
| Dual specificity protein phosphatase 5 | Homo sapiens (human) | Ki | 0.0250 | 1 | 1 |
| Ectonucleoside triphosphate diphosphohydrolase 1 | Rattus norvegicus (Norway rat) | Ki | 300.0000 | 2 | 2 |
| Ectonucleoside triphosphate diphosphohydrolase 2 | Rattus norvegicus (Norway rat) | Ki | 65.4000 | 2 | 2 |
| Ectonucleoside triphosphate diphosphohydrolase 3 | Rattus norvegicus (Norway rat) | Ki | 12.7000 | 1 | 1 |
| Ectonucleoside triphosphate diphosphohydrolase 8 | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| NAD-dependent protein deacetylase HST2 | Saccharomyces cerevisiae S288C | IC50 | 240.0000 | 1 | 1 |
| NAD-dependent protein deacetylase sirtuin-1 | Homo sapiens (human) | IC50 | 1.3857 | 7 | 7 |
| NAD-dependent protein deacetylase sirtuin-2 | Homo sapiens (human) | IC50 | 1.1750 | 4 | 4 |
| NAD-dependent protein deacylase sirtuin-5, mitochondrial | Homo sapiens (human) | IC50 | 20.6000 | 8 | 8 |
| P2X purinoceptor 2 | Rattus norvegicus (Norway rat) | IC50 | 21.9054 | 1 | 2 |
| P2Y purinoceptor 11 | Homo sapiens (human) | Ki | 0.2071 | 2 | 2 |
| P2Y purinoceptor 2 | Homo sapiens (human) | IC50 | 75.0000 | 2 | 2 |
| P2Y purinoceptor 6 | Homo sapiens (human) | IC50 | 27.0000 | 1 | 1 |
| Protein arginine N-methyltransferase 1 | Homo sapiens (human) | IC50 | 344.8100 | 3 | 3 |
| Protein kinase C alpha type | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Protein kinase C beta type | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Protein kinase C delta type | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Protein kinase C epsilon type | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Protein kinase C eta type | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Protein kinase C gamma type | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Protein kinase C iota type | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Protein kinase C theta type | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Protein kinase C zeta type | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | IC50 | 12.2000 | 2 | 2 |
| RmtA | Aspergillus nidulans | IC50 | 5.9000 | 1 | 1 |
| Serine/threonine-protein kinase D1 | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Serine/threonine-protein kinase D3 | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| Signal transducer and activator of transcription 1-alpha/beta | Homo sapiens (human) | IC50 | 9.1000 | 1 | 1 |
| Signal transducer and activator of transcription 3 | Mus musculus (house mouse) | IC50 | 100.0000 | 1 | 1 |
| Signal transducer and activator of transcription 5A | Homo sapiens (human) | IC50 | 9.4000 | 1 | 1 |
| Signal transducer and activator of transcription 5B | Homo sapiens (human) | IC50 | 10.4000 | 1 | 1 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 | 9.7600 | 1 | 1 |
| Uracil nucleotide/cysteinyl leukotriene receptor | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Delta-type opioid receptor | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
| Kappa-type opioid receptor | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
| Nuclear receptor subfamily 1 group I member 2 | Homo sapiens (human) | EC50 | 1.3000 | 1 | 1 |
| P2X purinoceptor 1 | Rattus norvegicus (Norway rat) | EC50 | 1.0000 | 1 | 1 |
| P2X purinoceptor 2 | Rattus norvegicus (Norway rat) | EC50 | 10.4000 | 1 | 1 |
| P2X purinoceptor 3 | Homo sapiens (human) | EC50 | 8.9500 | 2 | 2 |
| P2X purinoceptor 4 | Rattus norvegicus (Norway rat) | EC50 | 100.0000 | 1 | 1 |
| P2X purinoceptor 5 | Rattus norvegicus (Norway rat) | EC50 | 4.0000 | 1 | 1 |
| P2X purinoceptor 6 | Rattus norvegicus (Norway rat) | EC50 | 100.0000 | 1 | 1 |
| P2X purinoceptor 7 | Homo sapiens (human) | EC50 | 92.0000 | 1 | 1 |
| P2Y purinoceptor 1 | Meleagris gallopavo (turkey) | EC50 | 10.0000 | 1 | 1 |
| P2Y purinoceptor 11 | Homo sapiens (human) | EC50 | 16.0000 | 1 | 1 |
| P2Y purinoceptor 12 | Rattus norvegicus (Norway rat) | EC50 | 4.0000 | 1 | 1 |
| P2Y purinoceptor 2 | Homo sapiens (human) | EC50 | 48.0000 | 1 | 1 |
| P2Y purinoceptor 4 | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |