An antagonist at any adenosine receptor.
ChEBI ID: 71232
| 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 |
| theobromine | A dimethylxanthine having the two methyl groups located at positions 3 and 7. A purine alkaloid derived from the cacao plant, it is found in chocolate, as well as in a number of other foods, and is a vasodilator, diuretic and heart stimulator. | theobromine |
| theophylline | A dimethylxanthine having the two methyl groups located at positions 1 and 3. It is structurally similar to caffeine and is found in green and black tea. | theophylline |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 18,991 (44.91) | 18.7374 |
| 1990's | 7,997 (18.91) | 18.2507 |
| 2000's | 6,590 (15.58) | 29.6817 |
| 2010's | 6,395 (15.12) | 24.3611 |
| 2020's | 2,312 (5.47) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 4,179 (8.81%) | 5.53% |
| Reviews | 3,137 (6.61%) | 6.00% |
| Case Studies | 1,473 (3.10%) | 4.05% |
| Observational | 62 (0.13%) | 0.25% |
| Other | 38,590 (81.34%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| AR protein | Homo sapiens (human) | Potency | 33.3442 | 7 | 8 |
| arylsulfatase A | Homo sapiens (human) | Potency | 19.0090 | 1 | 2 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 23.3910 | 1 | 3 |
| atrial natriuretic peptide receptor 1 precursor | Homo sapiens (human) | Potency | 4.7755 | 1 | 1 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 2.5119 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 41.4299 | 1 | 3 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 25.1189 | 2 | 2 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 79.4328 | 1 | 1 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 11.9173 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 51.1148 | 6 | 7 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 46.4696 | 4 | 4 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 7.5360 | 1 | 8 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 24.2694 | 4 | 7 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 22.1430 | 1 | 1 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 33.1734 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 0.7450 | 1 | 2 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 17.9560 | 2 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 23.6916 | 1 | 3 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 1.3505 | 2 | 2 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 55.1482 | 1 | 1 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 3.1623 | 2 | 2 |
| IDH1 | Homo sapiens (human) | Potency | 20.5962 | 1 | 1 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 1.0177 | 1 | 3 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 0.0040 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.0234 | 1 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 31.3828 | 2 | 4 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 42.1632 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 15.8489 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 52.8242 | 2 | 3 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 37.9330 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 0.0029 | 1 | 1 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 84.9214 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 72.6796 | 1 | 2 |
| polyprotein | Zika virus | Potency | 33.1734 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 41.7461 | 1 | 2 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 15.8100 | 2 | 3 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 54.0104 | 2 | 5 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 19.5726 | 3 | 6 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 9.4411 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 1 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 23.8692 | 3 | 5 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 0.0014 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 18.1748 | 2 | 2 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 18.3701 | 2 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 55.6206 | 1 | 1 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 21.8724 | 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 |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Ki | 86.0000 | 1 | 1 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 7.2500 | 1 | 1 |
| Adenosine receptor A1 | Bos taurus (cattle) | IC50 | 1,006,650,005.0433 | 3 | 3 |
| Adenosine receptor A1 | Homo sapiens (human) | IC50 | 17.1040 | 1 | 1 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | IC50 | 66.2500 | 3 | 4 |
| Adenosine receptor A1 | Bos taurus (cattle) | Ki | 4.1143 | 7 | 7 |
| Adenosine receptor A1 | Cavia porcellus (domestic guinea pig) | Ki | 57.0909 | 7 | 11 |
| Adenosine receptor A1 | Gallus gallus (chicken) | Ki | 6.0000 | 1 | 1 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 19.7278 | 28 | 33 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | Ki | 23.7858 | 42 | 71 |
| Adenosine receptor A2a | Homo sapiens (human) | IC50 | 16.2395 | 1 | 2 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | IC50 | 63.0000 | 1 | 5 |
| Adenosine receptor A2a | Cavia porcellus (domestic guinea pig) | Ki | 35.6000 | 3 | 5 |
| Adenosine receptor A2a | Homo sapiens (human) | Ki | 13.7803 | 38 | 48 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | Ki | 94.8753 | 32 | 64 |
| Adenosine receptor A2b | Rattus norvegicus (Norway rat) | IC50 | 63.0000 | 1 | 5 |
| Adenosine receptor A2b | Homo sapiens (human) | Ki | 18.4318 | 29 | 38 |
| Adenosine receptor A2b | Mus musculus (house mouse) | Ki | 23.0000 | 1 | 1 |
| Adenosine receptor A2b | Rattus norvegicus (Norway rat) | Ki | 38.8394 | 20 | 47 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 47.4067 | 28 | 32 |
| Adenosine receptor A3 | Rattus norvegicus (Norway rat) | Ki | 49.9100 | 9 | 15 |
| Alkaline phosphatase, tissue-nonspecific isozyme | Homo sapiens (human) | IC50 | 52.5000 | 2 | 2 |
| Alkaline phosphatase, tissue-nonspecific isozyme | Homo sapiens (human) | Ki | 82.0000 | 1 | 1 |
| 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 | 2 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 307.2000 | 3 | 5 |
| 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 1A | Homo sapiens (human) | IC50 | 320.0000 | 1 | 1 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A | Bos taurus (cattle) | IC50 | 340.4000 | 5 | 5 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B | Bos taurus (cattle) | IC50 | 300.5000 | 4 | 4 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B | Homo sapiens (human) | IC50 | 320.0000 | 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 | Homo sapiens (human) | IC50 | 320.0000 | 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 | 608.8000 | 4 | 5 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Homo sapiens (human) | Ki | 530.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Rattus norvegicus (Norway rat) | Ki | 530.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Homo sapiens (human) | IC50 | 527.7500 | 4 | 4 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Homo sapiens (human) | Ki | 530.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Rattus norvegicus (Norway rat) | Ki | 530.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4C | Homo sapiens (human) | IC50 | 637.0000 | 3 | 3 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4C | Homo sapiens (human) | Ki | 530.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4C | Rattus norvegicus (Norway rat) | Ki | 530.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Homo sapiens (human) | IC50 | 637.0000 | 3 | 3 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Homo sapiens (human) | Ki | 530.0000 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Rattus norvegicus (Norway rat) | Ki | 530.0000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| Carbonic anhydrase 1 | Homo sapiens (human) | IC50 | 28,500.0000 | 1 | 2 |
| Carbonic anhydrase 2 | Homo sapiens (human) | IC50 | 28,500.0000 | 1 | 2 |
| cGMP-dependent 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 | 210.0000 | 1 | 1 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Homo sapiens (human) | IC50 | 300.0000 | 2 | 2 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) | IC50 | 300.0000 | 2 | 2 |
| Chain A, Chitinase | Clonostachys rosea | Ki | 19,700.0000 | 1 | 1 |
| Chain A, Glycogen Phosphorylase | Oryctolagus cuniculus (rabbit) | Ki | 100.0000 | 1 | 1 |
| Chain A, Pyridoxal kinase | Homo sapiens (human) | Ki | 50.0000 | 1 | 2 |
| Chitotriosidase-1 | Homo sapiens (human) | IC50 | 681.5000 | 1 | 4 |
| Cholinesterase | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| D(3) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 0.0006 | 1 | 1 |
| DNA-dependent protein kinase catalytic subunit | Homo sapiens (human) | IC50 | 10,000.0000 | 1 | 1 |
| Endochitinase B1 | Aspergillus fumigatus | IC50 | 681.5000 | 1 | 4 |
| 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 |
| High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| Intestinal-type alkaline phosphatase | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| 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 | 3,267.0000 | 1 | 2 |
| Phosphodiesterase | Bos taurus (cattle) | IC50 | 250.3333 | 6 | 6 |
| Phosphodiesterase | Rattus norvegicus (Norway rat) | IC50 | 70.0000 | 1 | 1 |
| Phosphodiesterase | Bos taurus (cattle) | Ki | 77.0000 | 1 | 1 |
| Phospholipase A-2-activating protein | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| Renin | Homo sapiens (human) | Ki | 6.5500 | 1 | 3 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 100.0000 | 1 | 2 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | IC50 | 100.0000 | 1 | 2 |
| 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 mTOR | Homo sapiens (human) | IC50 | 400.0000 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Cavia porcellus (domestic guinea pig) | Ki | 7.9000 | 1 | 1 |
| Thyroid hormone receptor beta | Rattus norvegicus (Norway rat) | Ki | 14.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Adenosine receptor A1 | Homo sapiens (human) | Kd | 28.5000 | 1 | 2 |
| Adenosine receptor A2a | Homo sapiens (human) | EC50 | 28.2000 | 1 | 1 |
| Adenosine receptor A2a | Homo sapiens (human) | Kd | 7.8127 | 3 | 5 |
| Chain A, glycogen phosphorylase, liver form | Homo sapiens (human) | Kd | 100.0000 | 1 | 8 |
| Palmitoleoyl-protein carboxylesterase NOTUM | Homo sapiens (human) | EC50 | 45.8000 | 1 | 1 |
| Palmitoleoyl-protein carboxylesterase NOTUM | Homo sapiens (human) | Kd | 3,442.5000 | 1 | 2 |
| Potassium channel subfamily K member 2 | Homo sapiens (human) | EC50 | 431.5000 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Adenosine receptor A1 | Homo sapiens (human) | Affinity constant | 20.0000 | 1 | 2 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | Kb | 49.7400 | 2 | 5 |
| Adenosine receptor A1 | Homo sapiens (human) | KD hydro | 76,250.0000 | 1 | 2 |
| Adenosine receptor A2a | Homo sapiens (human) | Affinity constant | 20.0000 | 1 | 2 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | Kb | 24.8500 | 2 | 2 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | Ratio | 36.5000 | 1 | 4 |
| Adenosine receptor A2b | Homo sapiens (human) | Affinity constant | 20.0000 | 1 | 2 |
| Adenosine receptor A2b | Mus musculus (house mouse) | Kb | 20.5000 | 2 | 2 |
| Adenosine receptor A2b | Rattus norvegicus (Norway rat) | Ratio | 36.5000 | 1 | 4 |
| Adenylate cyclase type 1 | Homo sapiens (human) | Kb | 22.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor | Cavia porcellus (domestic guinea pig) | Kb | 25.0000 | 1 | 1 |
| Vasopressin V2 receptor | Sus scrofa (pig) | Kb | 22.0000 | 1 | 2 |