An antagonist at the A2A receptor.
| Member | Definition | Class |
|---|
| 8-(3-chlorostyryl)caffeine | Caffeine substituted at its 8-position by an (E)-3-chlorostyryl group. | 8-(3-chlorostyryl)caffeine |
| 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 |
| cgs 15943 | A member of the class of triazoloquinazolines that is [1,2,4]triazolo[1,5-c]quinazoline substited at positions 2, 5 and 9 by furan-2-yl, amino and chloro groups respectively. A potent antagonist at adenosine A1 and adenosine A2A receptors. | 9-chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine; CGS 15943 |
| cyclazosin | A monocarboxylic acid amide obtained by formal condensation of the carboxy group of furoic acid with the secondary amino group of 6,7-dimethoxy-2-[(4aR,8aS)-octahydroquinoxalin-1-yl]quinazolin-4-amine. | cyclazosin |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 1.4125 | 1 | 1 |
| 2,3-bisphosphoglycerate-independent phosphoglycerate mutase | Leishmania major strain Friedlin | Potency | 21.3313 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 2.8797 | 1 | 2 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 4.8022 | 1 | 2 |
| AR protein | Homo sapiens (human) | Potency | 38.1074 | 7 | 7 |
| arylsulfatase A | Homo sapiens (human) | Potency | 9.6688 | 1 | 2 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 17.7957 | 2 | 2 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 42.5615 | 1 | 1 |
| atrial natriuretic peptide receptor 1 precursor | Homo sapiens (human) | Potency | 4.7755 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 14.1254 | 2 | 2 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 13.5346 | 1 | 2 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 19.9526 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 36.6418 | 2 | 3 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 72.3342 | 1 | 2 |
| CREB-binding protein | Homo sapiens (human) | Potency | 10.5785 | 3 | 3 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 7.9433 | 2 | 2 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 3.8046 | 2 | 2 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 18.4927 | 1 | 1 |
| DNA dC->dU-editing enzyme APOBEC-3G isoform 1 | Homo sapiens (human) | Potency | 0.5957 | 1 | 1 |
| 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 | 56.4950 | 6 | 6 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 38.6395 | 5 | 5 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 8.7487 | 1 | 6 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 22.1430 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 5.1156 | 2 | 2 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 17.9560 | 2 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 0.0178 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 55.1482 | 1 | 1 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 31.6228 | 1 | 3 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 65.8114 | 1 | 2 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 5.0119 | 2 | 2 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 8.9125 | 1 | 1 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 4.9494 | 1 | 3 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 31.0249 | 2 | 3 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 3.9811 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.0355 | 1 | 1 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 35.4813 | 1 | 1 |
| Nrf2 | Homo sapiens (human) | Potency | 1.4581 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 16.3642 | 2 | 2 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 8.1411 | 1 | 3 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 65.6524 | 2 | 2 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 66.6082 | 1 | 2 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 89.1251 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 5.5148 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 23.2944 | 2 | 2 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 12.8297 | 1 | 3 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 69.4275 | 2 | 3 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 19.7349 | 1 | 1 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 13.0099 | 3 | 3 |
| TDP1 protein | Homo sapiens (human) | Potency | 4.5502 | 2 | 6 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 19.4300 | 4 | 8 |
| Thrombopoietin | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 18.7232 | 2 | 2 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 0.0010 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 18.1748 | 2 | 2 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 112.2020 | 1 | 1 |
| 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 | 50.1187 | 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 | 1.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 1 | 1 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 7.2500 | 1 | 1 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | IC50 | 56.7611 | 3 | 4 |
| Adenosine receptor A1 | Cavia porcellus (domestic guinea pig) | Ki | 83.3350 | 5 | 6 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 30.0838 | 18 | 18 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | Ki | 30.8143 | 36 | 43 |
| Adenosine receptor A2a | Homo sapiens (human) | IC50 | 10.2420 | 2 | 2 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | IC50 | 28.6379 | 2 | 11 |
| Adenosine receptor A2a | Cavia porcellus (domestic guinea pig) | Ki | 50.0000 | 3 | 3 |
| Adenosine receptor A2a | Homo sapiens (human) | Ki | 10.2604 | 39 | 42 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | Ki | 117.8422 | 34 | 41 |
| Adenosine receptor A2b | Homo sapiens (human) | IC50 | 0.6304 | 2 | 2 |
| Adenosine receptor A2b | Rattus norvegicus (Norway rat) | IC50 | 31.5014 | 1 | 10 |
| Adenosine receptor A2b | Homo sapiens (human) | Ki | 19.1503 | 25 | 27 |
| 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) | IC50 | 0.4060 | 1 | 1 |
| Adenosine receptor A3 | Rattus norvegicus (Norway rat) | IC50 | 0.0607 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 16.4528 | 31 | 31 |
| Adenosine receptor A3 | Rattus norvegicus (Norway rat) | Ki | 56.6667 | 6 | 6 |
| Alpha-1A adrenergic receptor | Bos taurus (cattle) | Ki | 0.0024 | 1 | 1 |
| Alpha-1A adrenergic receptor | Homo sapiens (human) | Ki | 0.0138 | 4 | 4 |
| Alpha-1A adrenergic receptor | Oryctolagus cuniculus (rabbit) | Ki | 0.0251 | 1 | 1 |
| Alpha-1B adrenergic receptor | Homo sapiens (human) | Ki | 0.0003 | 6 | 6 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.0003 | 1 | 1 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Ki | 0.0096 | 4 | 4 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.0006 | 1 | 1 |
| Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.0316 | 1 | 3 |
| Alpha-2B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.0316 | 1 | 3 |
| Alpha-2C adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.0316 | 1 | 3 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | IC50 | 23.3333 | 3 | 3 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | IC50 | 10.1283 | 5 | 5 |
| Amine oxidase [flavin-containing] B | Rattus norvegicus (Norway rat) | IC50 | 0.0385 | 1 | 1 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | Ki | 925.0977 | 7 | 8 |
| Amine oxidase [flavin-containing] B | Mus musculus (house mouse) | Ki | 0.1000 | 1 | 1 |
| Amine oxidase [flavin-containing] B | Rattus norvegicus (Norway rat) | Ki | 0.2100 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Beta-casein | Rattus norvegicus (Norway rat) | Ki | 0.0001 | 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 |
| Casein kinase I isoform alpha | Homo sapiens (human) | IC50 | 0.8200 | 1 | 1 |
| Casein kinase I isoform delta | Homo sapiens (human) | IC50 | 0.2400 | 1 | 1 |
| Casein kinase I isoform epsilon | Homo sapiens (human) | IC50 | 0.4900 | 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 |
| Cytochrome P450 11B1, mitochondrial | Rattus norvegicus (Norway rat) | Ki | 0.0044 | 1 | 1 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0004 | 1 | 1 |
| DNA-dependent protein kinase catalytic subunit | Homo sapiens (human) | IC50 | 5,000.0700 | 2 | 2 |
| 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 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0004 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 0.0123 | 1 | 1 |
| Palmitoleoyl-protein carboxylesterase NOTUM | Homo sapiens (human) | IC50 | 18.6000 | 1 | 1 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | Homo sapiens (human) | IC50 | 1.2800 | 1 | 1 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform | Homo sapiens (human) | IC50 | 8.4800 | 1 | 1 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | Homo sapiens (human) | IC50 | 0.9700 | 1 | 1 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | Homo sapiens (human) | IC50 | 1,815.0550 | 2 | 2 |
| Phosphodiesterase | Rattus norvegicus (Norway rat) | IC50 | 70.0000 | 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 |
| 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 |