A ryanodine receptor modulator which activates the receptor. Ryanodine receptors (RyRs) act as selective ion channels, modulating the release of calcium. Activating the receptors causes the release of calcium, so depleting internal calcium and ultimately preventing further muscle contraction.
| Member | Definition | Class |
|---|
| caffeine | A trimethylxanthine in which the three methyl groups are located at positions 1, 3, and 7. A purine alkaloid that occurs naturally in tea and coffee. | caffeine |
| chlorantranilipole | A carboxamide resulting from the formal condensation of the carboxylic acid group of 3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxylic acid with the primary amino group of 2-amino-5-chloro-N,3-dimethylbenzamide. The first of the anthranilic diamide insecticides, it is a ryanodine receptor activator and is used to protect a wide variety of crops, including corn, cotton, grapes, rice and potatoes. | chlorantraniliprole |
| chlorocresol | A hydroxytoluene that is 3-methylphenol which is substituted by a chlorine at position 4. A ryanodine receptor agonist. | 4-chloro-m-cresol |
| cyantraniliprole | A carboxamide that is chlorantraniliprole in which the chlorine atom attached to the phenyl ring has been replaced by a cyano group. A ryanodine receptor agonist, it is used as insecticide for the control of whitefly, thrips, aphids, fruitflies, and fruit worms in crops such as onions, potatoes and tomatoes. It is highly toxic to honeybees. | cyantraniliprole |
| cyclic adp-ribose | A cyclic purine nucleotide that is synthesised from NAD+ by ADP-ribosyl cyclase; acts as an agonist at ryanodine receptors. | cyclic ADP-beta-D-ribose |
| 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 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| AR protein | Homo sapiens (human) | Potency | 39.5188 | 7 | 8 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 35.2410 | 2 | 2 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 24.8205 | 2 | 2 |
| atrial natriuretic peptide receptor 1 precursor | Homo sapiens (human) | Potency | 4.7755 | 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, Ferritin light chain | Equus caballus (horse) | Potency | 14.1254 | 1 | 1 |
| 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, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 15.8114 | 1 | 1 |
| 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 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 17.3768 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 27.5404 | 1 | 1 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 40.1620 | 1 | 2 |
| 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 | 4.0163 | 1 | 3 |
| endonuclease IV | Escherichia coli | Potency | 9.2961 | 2 | 2 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 50.3995 | 8 | 11 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 63.8522 | 4 | 4 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 3.8192 | 1 | 5 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 10.4760 | 2 | 2 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 22.1430 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 17.3768 | 1 | 1 |
| galactokinase | Homo sapiens (human) | Potency | 17.7828 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 0.2311 | 1 | 1 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 14.5360 | 2 | 3 |
| GLS protein | Homo sapiens (human) | Potency | 22.1969 | 2 | 2 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 25.0682 | 1 | 2 |
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | Potency | 8.9125 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 32.0304 | 2 | 2 |
| 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 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 17.3768 | 1 | 1 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 17.3768 | 1 | 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 |
| Interferon beta | Homo sapiens (human) | Potency | 17.3768 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 2.3877 | 2 | 2 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 1.1294 | 1 | 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 | 0.8102 | 1 | 2 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 0.3548 | 2 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 33.1842 | 3 | 3 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 21.1317 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 23.7358 | 2 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 60.6574 | 3 | 5 |
| Ornithine decarboxylase | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 36.1254 | 1 | 1 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 10.5901 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 66.0676 | 1 | 3 |
| 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 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 5.5148 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 3.3491 | 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 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 15.5458 | 2 | 3 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 0.0075 | 1 | 1 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 69.4275 | 2 | 3 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 14.1279 | 2 | 3 |
| 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 hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 21.5842 | 3 | 3 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 0.0014 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 12.2422 | 4 | 4 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 35.5195 | 1 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 55.6206 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 55.1482 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 7.2500 | 1 | 1 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | IC50 | 113.5000 | 2 | 2 |
| Adenosine receptor A1 | Cavia porcellus (domestic guinea pig) | Ki | 100.0000 | 5 | 5 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 35.4333 | 15 | 15 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | Ki | 37.5909 | 30 | 33 |
| Adenosine receptor A2a | Homo sapiens (human) | IC50 | 20.4720 | 1 | 1 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | IC50 | 63.0000 | 1 | 5 |
| Adenosine receptor A2a | Cavia porcellus (domestic guinea pig) | Ki | 50.0000 | 3 | 3 |
| Adenosine receptor A2a | Homo sapiens (human) | Ki | 20.5069 | 21 | 21 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | Ki | 160.9033 | 25 | 30 |
| Adenosine receptor A2b | Rattus norvegicus (Norway rat) | IC50 | 63.0000 | 1 | 5 |
| Adenosine receptor A2b | Homo sapiens (human) | Ki | 26.7211 | 19 | 19 |
| Adenosine receptor A2b | Mus musculus (house mouse) | Ki | 23.0000 | 1 | 1 |
| Adenosine receptor A2b | Rattus norvegicus (Norway rat) | Ki | 35.3050 | 15 | 20 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 34.9750 | 12 | 12 |
| Adenosine receptor A3 | Rattus norvegicus (Norway rat) | Ki | 56.6667 | 6 | 6 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | Ki | 3,700.0000 | 2 | 2 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| ATP-dependent 6-phosphofructokinase | Trypanosoma brucei brucei | IC50 | 3.0000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 422.6667 | 3 | 3 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 | 14,000.0000 | 1 | 1 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B | Rattus norvegicus (Norway rat) | IC50 | 70.0000 | 1 | 1 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C | Rattus norvegicus (Norway rat) | IC50 | 70.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Homo sapiens (human) | IC50 | 747.0000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Carbonic anhydrase 1 | Homo sapiens (human) | IC50 | 28,500.0000 | 1 | 2 |
| Carbonic anhydrase 2 | Homo sapiens (human) | IC50 | 28,500.0000 | 1 | 2 |
| Cathepsin B | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| Chain A, Chitinase | Clonostachys rosea | Ki | 19,700.0000 | 1 | 1 |
| Chain A, Glycogen Phosphorylase | Oryctolagus cuniculus (rabbit) | Ki | 100.0000 | 1 | 1 |
| Chitotriosidase-1 | Homo sapiens (human) | IC50 | 363.0000 | 1 | 2 |
| Cholinesterase | Homo sapiens (human) | IC50 | 50.0000 | 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 | 5,000.8500 | 2 | 2 |
| 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 |
| Endochitinase B1 | Aspergillus fumigatus | IC50 | 363.0000 | 1 | 2 |
| Glycogen phosphorylase, liver form | Rattus norvegicus (Norway rat) | IC50 | 648.0000 | 1 | 1 |
| Glycogen phosphorylase, muscle form | Oryctolagus cuniculus (rabbit) | IC50 | 159.1933 | 13 | 15 |
| Glycogen phosphorylase, muscle form | Rattus norvegicus (Norway rat) | IC50 | 182.0000 | 1 | 1 |
| Guanine deaminase | Homo sapiens (human) | Ki | 10.2000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 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 |
| Palmitoleoyl-protein carboxylesterase NOTUM | Homo sapiens (human) | IC50 | 18.6000 | 1 | 1 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | Homo sapiens (human) | IC50 | 3,630.0000 | 1 | 1 |
| Phosphodiesterase | Rattus norvegicus (Norway rat) | IC50 | 70.0000 | 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 |
| Renin | Homo sapiens (human) | Ki | 15.0000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 100.0000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | IC50 | 100.0000 | 1 | 1 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | IC50 | 12.2000 | 2 | 2 |
| RmtA | Aspergillus nidulans | IC50 | 5.9000 | 1 | 1 |
| Ryanodine receptor | Bemisia tabaci | IC50 | 0.0020 | 1 | 1 |
| Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 | Oryctolagus cuniculus (rabbit) | IC50 | 2,800.0000 | 1 | 1 |
| Serine-protein kinase ATM | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| Serine/threonine-protein kinase ATR | Homo sapiens (human) | IC50 | 1,100.0000 | 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 |
| Serine/threonine-protein kinase mTOR | Homo sapiens (human) | IC50 | 400.0000 | 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 |