An antagonist at the A1 receptor.
| Member | Definition | Class |
|---|
| 1,3-dipropyl-8-cyclopentylxanthine | An oxopurine that is 7H-xanthine substituted at positions 1 and 3 by propyl groups and at position 8 by a cyclohexyl group. | DPCPX |
| 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 |
| sulmazole | An imidazopyridine that is 1H-imidazo[4,5-b]pyridine which is substituted at position 2 by a 2-methoxy-4-(methylsulfinyl)phenyl group. An A1 adenosine receptor antagonist, it was formerly used as a cardiotonic agent. | sulmazole |
| swertisin | A flavone C-glycoside that is 7-O-methylapigenin in which the hydrogen at position 6 has been replaced by a beta-D-glucosyl residue. | swertisin |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 18.8541 | 1 | 2 |
| 2,3-bisphosphoglycerate-independent phosphoglycerate mutase | Leishmania major strain Friedlin | Potency | 21.3313 | 1 | 1 |
| 67.9K protein | Vaccinia virus | Potency | 10.0000 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 20.3866 | 1 | 2 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 2.1132 | 2 | 2 |
| arylsulfatase A | Homo sapiens (human) | Potency | 2.3934 | 1 | 1 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 17.9801 | 2 | 3 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 21.3284 | 1 | 3 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 10.0000 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 28.1838 | 1 | 1 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 18.9338 | 2 | 3 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 18.9338 | 2 | 3 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 89.7164 | 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 iota isoform a (long) | Homo sapiens (human) | Potency | 0.4467 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 18.6371 | 2 | 4 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 3.6548 | 1 | 3 |
| 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 | 11.8341 | 3 | 4 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 31.6228 | 1 | 3 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 20.5348 | 1 | 2 |
| 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 | 7.5060 | 2 | 4 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 15.6001 | 2 | 4 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 12.5893 | 1 | 1 |
| 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 | 22.3872 | 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 2 | Homo sapiens (human) | Potency | 23.1093 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 14.6852 | 2 | 3 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 61.4272 | 1 | 2 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 0.6695 | 1 | 1 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 13.0099 | 3 | 3 |
| TDP1 protein | Homo sapiens (human) | Potency | 4.4234 | 2 | 7 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 39.8571 | 3 | 6 |
| Thrombopoietin | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 0.0006 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 6.3096 | 2 | 2 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 60.4566 | 2 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Ki | 1.0295 | 2 | 2 |
| Adenosine receptor A1 | Homo sapiens (human) | IC50 | 0.0083 | 9 | 9 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | IC50 | 0.0054 | 3 | 4 |
| Adenosine receptor A1 | Bos taurus (cattle) | Ki | 0.0005 | 8 | 8 |
| Adenosine receptor A1 | Cavia porcellus (domestic guinea pig) | Ki | 0.0064 | 8 | 9 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 19,908.1323 | 48 | 50 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | Ki | 0.0036 | 28 | 39 |
| Adenosine receptor A2a | Homo sapiens (human) | IC50 | 0.1555 | 4 | 4 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | IC50 | 0.0029 | 2 | 6 |
| Adenosine receptor A2a | Homo sapiens (human) | Ki | 11,232.1463 | 58 | 66 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | Ki | 0.3753 | 23 | 31 |
| Adenosine receptor A2b | Homo sapiens (human) | IC50 | 0.3269 | 3 | 4 |
| Adenosine receptor A2b | Rattus norvegicus (Norway rat) | IC50 | 0.0028 | 1 | 5 |
| Adenosine receptor A2b | Homo sapiens (human) | Ki | 0.4458 | 24 | 24 |
| Adenosine receptor A2b | Rattus norvegicus (Norway rat) | Ki | 0.3352 | 11 | 16 |
| Adenosine receptor A3 | Homo sapiens (human) | IC50 | 0.4060 | 1 | 1 |
| Adenosine receptor A3 | Rattus norvegicus (Norway rat) | IC50 | 0.0322 | 1 | 2 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 3.0094 | 50 | 56 |
| Adenosine receptor A3 | Rattus norvegicus (Norway rat) | Ki | 3.2950 | 2 | 2 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| 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 |
| cGMP-dependent 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Homo sapiens (human) | IC50 | 383.3333 | 3 | 3 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) | IC50 | 383.3333 | 3 | 3 |
| cGMP-specific 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 | 21.0000 | 1 | 1 |
| Cytochrome P450 11B1, mitochondrial | Rattus norvegicus (Norway rat) | Ki | 0.0044 | 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 | 0.1400 | 1 | 1 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0004 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 100.0000 | 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 | 0.1100 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Cavia porcellus (domestic guinea pig) | Ki | 0.2600 | 1 | 1 |