Page last updated: 2024-08-05 15:33:50
estrogen receptor antagonist
An antagonist at the estrogen receptor.
ChEBI ID: 50792
Members (9)
| Member | Definition | Class |
|---|---|---|
| 5,11-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol | A carbotetracyclic compound that is 5,6,11,12-tetrahydrochrysene substituted by hydroxy groups at positions 2 and 8 and by ethyl groups at positions 5 and 11 (the 5R,11R-stereoisomer). It is an agonist of ER-alpha and antagonist of ER-beta receptors. | (R,R)-5,11-diethyl-5,6,11,12-tetrahydro-2,8-chrysenediol |
| afimoxifene | A tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen. | afimoxifene |
| diallyl trisulfide | An organic trisulfide that is trisulfane in which both of the hydrogens are replaced by allyl groups. A component of the essential oil of garlic and a major component of the traditional Chinese medicine allitridium, it exhibits antifungal, antitumour and antioxidant activity | diallyl trisulfide |
| fulvestrant | A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer. | fulvestrant |
| ici 164384 | A 3-hydroxy steroid that is 17beta-estradiol substituted by a 11-[butyl(methyl)amino]-11-oxoundecyl group at position 7R. It is a steroidal antioestrogen that inhibits the cell proliferation of breast-carcinoma cell lines. | ICI-164384 |
| lasofoxifene | A member of the class of tetralins that is 5,6,7,8-tetrahydronaphthalen-2-ol in which the hydrogens at positions 5 and 6 are replaced by 4-[2-(pyrrolidin-1-yl)ethoxy]phenyl and phenyl groups, respectively (the 5R,6S-stereoisomer). It is a selective estrogen receptor modulator indicated for the prevention and treatment of osteoporosis in post-menopausal women. | lasofoxifene |
| ly 117018 | A member of the class of 1-benzothiophenes that is raloxifene in which the piperidin-1-yl group has been replaced by a pyrrolidin-1-yl group. | LY 117018 |
| ru 58668 | A 17beta-hydroxy steroid that is 17beta-estradiol in the the hydrogen at the 11beta position has been replaced by a p-({5-[(4,4,5,5,5-pentafluoropentyl)sulfonyl]pentyl}oxy)phenyl group. RU 58668 is a pure anti-estrogen that downregulates estrogen receptor expression (IC50 = 0.04 nM). | RU 58668 |
| tamoxifen | tamoxifen |
Research
Studies (22,134)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 2,520 (11.39) | 18.7374 |
| 1990's | 4,589 (20.73) | 18.2507 |
| 2000's | 6,851 (30.95) | 29.6817 |
| 2010's | 6,462 (29.19) | 24.3611 |
| 2020's | 1,712 (7.73) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 2,462 (9.69%) | 5.53% |
| Reviews | 3,049 (12.00%) | 6.00% |
| Case Studies | 1,303 (5.13%) | 4.05% |
| Observational | 74 (0.29%) | 0.25% |
| Other | 18,526 (72.90%) | 84.16% |
Protein Targets (275)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 29.3301 | 1 | 3 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| 67.9K protein | Vaccinia virus | Potency | 10.4510 | 1 | 3 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 59.5216 | 3 | 7 |
| acid sphingomyelinase | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 42.8427 | 2 | 7 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 22.9856 | 1 | 3 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 32.8152 | 3 | 5 |
| Alpha-synuclein | Homo sapiens (human) | Potency | 18.3564 | 1 | 2 |
| Amyloid-beta precursor protein | Homo sapiens (human) | Potency | 29.0929 | 1 | 1 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 35.4813 | 1 | 2 |
| AR protein | Homo sapiens (human) | Potency | 30.9548 | 10 | 29 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 25.7523 | 1 | 1 |
| arylsulfatase A | Homo sapiens (human) | Potency | 5.0669 | 1 | 2 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 23.9557 | 2 | 3 |
| Ataxin-2 | Homo sapiens (human) | Potency | 47.5969 | 2 | 5 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 69.2156 | 2 | 4 |
| atrial natriuretic peptide receptor 1 precursor | Homo sapiens (human) | Potency | 10.6910 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 17.7828 | 2 | 2 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 39.9868 | 1 | 3 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 41.0163 | 1 | 3 |
| caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 36.5558 | 1 | 3 |
| caspase-3 | Homo sapiens (human) | Potency | 41.0163 | 1 | 3 |
| Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 36.5558 | 1 | 3 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 42.2158 | 3 | 11 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 22.9210 | 2 | 4 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 26.6514 | 1 | 2 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 14.9867 | 2 | 3 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 28.1838 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 28.4542 | 2 | 4 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 25.1189 | 2 | 2 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 50.3404 | 1 | 3 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 100.0000 | 1 | 1 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 25.1189 | 2 | 2 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 35.6383 | 2 | 3 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 1.3803 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 35.7168 | 1 | 2 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 29.0941 | 2 | 6 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 1.5008 | 2 | 2 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 2.4293 | 1 | 5 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 4.1570 | 3 | 4 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 14.6892 | 1 | 1 |
| Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 100.0000 | 1 | 1 |
| DNA polymerase III, partial | Bacillus subtilis | Potency | 29.9349 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 64.0919 | 1 | 2 |
| dopamine D1 receptor | Homo sapiens (human) | Potency | 23.1093 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 14.6227 | 12 | 49 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 48.0423 | 3 | 12 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 23.5998 | 10 | 43 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 15.8783 | 1 | 9 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 44.3332 | 5 | 10 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 1.3803 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| GALC protein | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 29.0941 | 1 | 3 |
| geminin | Homo sapiens (human) | Potency | 16.3430 | 4 | 7 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 11.9463 | 3 | 12 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 18.0636 | 1 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 11.0705 | 2 | 3 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 25.6572 | 1 | 6 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 29.9233 | 4 | 13 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 1.4810 | 1 | 6 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 46.2917 | 2 | 5 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 5.2462 | 2 | 11 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 46.9920 | 2 | 5 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 1.3803 | 1 | 1 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 49.0905 | 2 | 6 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 25.1189 | 2 | 2 |
| IDH1 | Homo sapiens (human) | Potency | 17.0255 | 1 | 3 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 1.3803 | 1 | 2 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 23.7358 | 1 | 2 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 23.7358 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 22.9113 | 2 | 4 |
| isocitrate dehydrogenase 1, partial | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 23.8427 | 2 | 3 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 23.7358 | 1 | 2 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 28.3368 | 1 | 2 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 21.8112 | 2 | 6 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 23.7531 | 2 | 2 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 11.2947 | 2 | 2 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 10.0000 | 1 | 2 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 10.0000 | 2 | 2 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 10.6101 | 1 | 2 |
| NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 58.0479 | 1 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 34.3699 | 3 | 8 |
| nuclear factor NF-kappa-B p105 subunit isoform 1 | Homo sapiens (human) | Potency | 36.4261 | 1 | 2 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 36.1676 | 2 | 6 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 21.9774 | 2 | 6 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 28.1838 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 48.8568 | 3 | 10 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| Parkin | Homo sapiens (human) | Potency | 25.9290 | 1 | 1 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 37.9330 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 57.1173 | 5 | 10 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 40.2832 | 5 | 8 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 47.2838 | 2 | 6 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 5.3808 | 1 | 2 |
| polyprotein | Zika virus | Potency | 35.4813 | 1 | 1 |
| polyunsaturated fatty acid lipoxygenase ALOX12 | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 6.0276 | 1 | 4 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 30.0883 | 1 | 2 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 7.8161 | 3 | 8 |
| pregnane X receptor | Rattus norvegicus (Norway rat) | Potency | 55.5278 | 1 | 2 |
| progesterone receptor | Homo sapiens (human) | Potency | 44.9726 | 3 | 10 |
| putative alpha-glucosidase | Oryza sativa Japonica Group (Japanese rice) | Potency | 39.8107 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 20.1698 | 2 | 12 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 75.0238 | 1 | 2 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 15.2714 | 1 | 3 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 53.0278 | 3 | 9 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 34.0893 | 4 | 8 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 18.0949 | 4 | 5 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 61.1334 | 3 | 7 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 61.1334 | 3 | 7 |
| Smad3 | Homo sapiens (human) | Potency | 35.4813 | 1 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 1 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 21.0530 | 2 | 9 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 33.6681 | 4 | 9 |
| Thrombopoietin | Homo sapiens (human) | Potency | 5.0119 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 7.3522 | 3 | 11 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 16.4148 | 2 | 3 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 47.2922 | 6 | 10 |
| thyrotropin-releasing hormone receptor | Homo sapiens (human) | Potency | 29.4629 | 2 | 5 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| ubiquitin carboxyl-terminal hydrolase 2 isoform a | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 5.3808 | 1 | 2 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 5.3808 | 1 | 2 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 59.6649 | 1 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 22.2278 | 2 | 6 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 58.0621 | 4 | 5 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 39.2394 | 1 | 5 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 1.4810 | 1 | 6 |
| Vpr | Human immunodeficiency virus 1 | Potency | 35.4813 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Homo sapiens (human) | IC50 | 0.0120 | 1 | 1 |
| 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Homo sapiens (human) | Ki | 0.0050 | 1 | 1 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 | 12.1600 | 1 | 1 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 6.9490 | 1 | 1 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | IC50 | 12.1600 | 1 | 1 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | Ki | 6.9490 | 1 | 1 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | IC50 | 4.8010 | 1 | 1 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 1.3720 | 1 | 1 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | IC50 | 2.0840 | 1 | 1 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 1.3260 | 1 | 1 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 | 0.4600 | 1 | 1 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 0.2410 | 1 | 1 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | IC50 | 0.4600 | 1 | 1 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | Ki | 0.2410 | 1 | 1 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | IC50 | 2.6790 | 1 | 1 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | Ki | 1.1425 | 2 | 2 |
| 7-dehydrocholesterol reductase | Homo sapiens (human) | IC50 | 0.0120 | 1 | 1 |
| Adenosine receptor A1 | Homo sapiens (human) | IC50 | 23.7670 | 1 | 1 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 13.8640 | 1 | 1 |
| Adenosine receptor A2a | Homo sapiens (human) | IC50 | 7.0990 | 1 | 1 |
| Adenosine receptor A2a | Homo sapiens (human) | Ki | 3.9850 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | IC50 | 3.7010 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 2.0920 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | IC50 | 1.4720 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 1.4590 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 3.7010 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 2.0920 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 3.7010 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 2.0920 | 1 | 1 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | IC50 | 4.9820 | 1 | 1 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Ki | 2.4490 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 | 1.9350 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 0.7260 | 1 | 1 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | IC50 | 3.5180 | 1 | 1 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 1.6060 | 1 | 1 |
| Androgen receptor | Rattus norvegicus (Norway rat) | IC50 | 17.3423 | 2 | 2 |
| Androgen receptor | Rattus norvegicus (Norway rat) | Ki | 15.1080 | 1 | 1 |
| Angiotensin-converting enzyme | Oryctolagus cuniculus (rabbit) | IC50 | 0.9670 | 1 | 1 |
| Angiotensin-converting enzyme | Oryctolagus cuniculus (rabbit) | Ki | 0.7922 | 1 | 1 |
| Aromatase | Homo sapiens (human) | IC50 | 530.0000 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 | 19.7250 | 4 | 4 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
| B2 bradykinin receptor | Homo sapiens (human) | IC50 | 20.3560 | 1 | 1 |
| B2 bradykinin receptor | Homo sapiens (human) | Ki | 12.0480 | 1 | 1 |
| Beta-1 adrenergic receptor | Homo sapiens (human) | IC50 | 17.2890 | 1 | 1 |
| Beta-1 adrenergic receptor | Homo sapiens (human) | Ki | 9.9840 | 1 | 1 |
| Beta-3 adrenergic receptor | Homo sapiens (human) | IC50 | 7.7030 | 1 | 1 |
| Beta-3 adrenergic receptor | Homo sapiens (human) | Ki | 5.7780 | 1 | 1 |
| Beta-lactamase TEM | Escherichia coli | IC50 | 55.9000 | 1 | 1 |
| Bifunctional epoxide hydrolase 2 | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| Bifunctional epoxide hydrolase 2 | Homo sapiens (human) | Ki | 0.0260 | 1 | 1 |
| Bile acid receptor | Homo sapiens (human) | IC50 | 1.0500 | 1 | 2 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 74.9500 | 5 | 6 |
| C-8 sterol isomerase | Saccharomyces cerevisiae S288C | Ki | 1.5000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| Chain A, CES1 protein | Homo sapiens (human) | Ki | 15.2000 | 1 | 1 |
| Cytochrome P450 2B6 | Homo sapiens (human) | Ki | 0.9000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 0.2000 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | IC50 | 8.5020 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 4.2510 | 1 | 1 |
| D(2) dopamine receptor | Homo sapiens (human) | IC50 | 13.8850 | 1 | 1 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 4.6280 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | IC50 | 1.0720 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 0.3640 | 1 | 1 |
| D(4) dopamine receptor | Homo sapiens (human) | IC50 | 11.1610 | 1 | 1 |
| D(4) dopamine receptor | Homo sapiens (human) | Ki | 3.9130 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | IC50 | 13.3390 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 4.7020 | 1 | 1 |
| Emopamil-binding protein-like | Homo sapiens (human) | Ki | 0.0028 | 1 | 1 |
| Epidermal growth factor receptor | Homo sapiens (human) | IC50 | 3.5530 | 1 | 1 |
| Estrogen receptor | Homo sapiens (human) | IC50 | 0.4831 | 82 | 102 |
| Estrogen receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0094 | 2 | 3 |
| Estrogen receptor | Homo sapiens (human) | Ki | 0.0253 | 8 | 10 |
| Estrogen receptor beta | Homo sapiens (human) | IC50 | 0.5935 | 41 | 48 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | IC50 | 0.0112 | 1 | 2 |
| Estrogen receptor beta | Homo sapiens (human) | Ki | 0.0222 | 8 | 10 |
| Estrogen-related receptor gamma | Homo sapiens (human) | IC50 | 0.0219 | 3 | 4 |
| Fatty acid synthase | Gallus gallus (chicken) | IC50 | 8.3700 | 2 | 2 |
| Histamine H2 receptor | Homo sapiens (human) | IC50 | 9.3960 | 1 | 1 |
| Histamine H2 receptor | Homo sapiens (human) | Ki | 9.2400 | 1 | 1 |
| Kappa-type opioid receptor | Homo sapiens (human) | IC50 | 15.6290 | 1 | 1 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 6.2520 | 1 | 1 |
| Melanocortin receptor 3 | Homo sapiens (human) | IC50 | 19.8560 | 1 | 1 |
| Melanocortin receptor 3 | Homo sapiens (human) | Ki | 17.3290 | 1 | 1 |
| Melanocortin receptor 4 | Homo sapiens (human) | IC50 | 30.4810 | 1 | 1 |
| Melanocortin receptor 4 | Homo sapiens (human) | Ki | 29.3080 | 1 | 1 |
| Melanocortin receptor 5 | Homo sapiens (human) | IC50 | 26.5290 | 1 | 1 |
| Melanocortin receptor 5 | Homo sapiens (human) | Ki | 24.8860 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | IC50 | 17.5940 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 7.1420 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | IC50 | 2.8290 | 1 | 1 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Ki | 0.6810 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | IC50 | 7.7930 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 2.7710 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | IC50 | 2.9740 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 0.6300 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | IC50 | 4.8170 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 0.6720 | 1 | 1 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | IC50 | 2.5850 | 1 | 1 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Ki | 1.8570 | 1 | 1 |
| NAD-dependent protein deacylase sirtuin-5, mitochondrial | Homo sapiens (human) | IC50 | 2.6000 | 1 | 1 |
| Nuclear receptor subfamily 3 group C member 3 | Bos taurus (cattle) | IC50 | 0.9670 | 1 | 1 |
| Nuclear receptor subfamily 3 group C member 3 | Bos taurus (cattle) | Ki | 0.7922 | 1 | 1 |
| Phospholipase D1 | Homo sapiens (human) | IC50 | 15.5000 | 2 | 3 |
| Phospholipase D1 | Rattus norvegicus (Norway rat) | IC50 | 20.0000 | 1 | 1 |
| Phospholipase D2 | Homo sapiens (human) | IC50 | 13.2500 | 1 | 2 |
| Platelet-activating factor acetylhydrolase | Homo sapiens (human) | IC50 | 0.9040 | 1 | 1 |
| Polyunsaturated fatty acid 5-lipoxygenase | Homo sapiens (human) | Ki | 0.0262 | 3 | 7 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 1.2759 | 2 | 2 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Ki | 0.7922 | 1 | 1 |
| Progesterone receptor | Homo sapiens (human) | IC50 | 50.0323 | 2 | 4 |
| Prostaglandin G/H synthase 1 | Homo sapiens (human) | IC50 | 4.3910 | 1 | 1 |
| Protein kinase C alpha type | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Protein kinase C alpha type | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 1 | 1 |
| Protein kinase C beta type | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Protein kinase C beta type | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 1 | 1 |
| Protein kinase C delta type | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Protein kinase C delta type | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 1 | 1 |
| Protein kinase C epsilon type | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Protein kinase C epsilon type | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 1 | 1 |
| Protein kinase C eta type | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Protein kinase C eta type | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 1 | 1 |
| Protein kinase C gamma type | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Protein kinase C gamma type | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 1 | 1 |
| Protein kinase C iota type | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Protein kinase C theta type | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Protein kinase C theta type | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 1 | 1 |
| Protein kinase C zeta type | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Protein kinase C zeta type | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 1 | 1 |
| Receptor tyrosine-protein kinase erbB-2 | Homo sapiens (human) | IC50 | 2.9490 | 1 | 1 |
| Serine/threonine-protein kinase D1 | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Serine/threonine-protein kinase D3 | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoform | Homo sapiens (human) | IC50 | 30.5730 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | IC50 | 0.0210 | 1 | 1 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 0.0219 | 2 | 2 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | IC50 | 1.8410 | 1 | 1 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 1.4620 | 1 | 1 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 | 1.4720 | 1 | 1 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 1.4590 | 1 | 1 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | IC50 | 2.3340 | 1 | 1 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 1.2400 | 1 | 1 |
| Steroid hormone receptor ERR1 | Homo sapiens (human) | IC50 | 0.1010 | 1 | 2 |
| Substance-K receptor | Homo sapiens (human) | IC50 | 3.6700 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | Ki | 1.2230 | 1 | 1 |
| Substance-P receptor | Homo sapiens (human) | IC50 | 15.6560 | 1 | 1 |
| Substance-P receptor | Homo sapiens (human) | Ki | 8.5400 | 1 | 1 |
| Thromboxane-A synthase | Homo sapiens (human) | IC50 | 0.9160 | 1 | 1 |
| Transcriptional activator protein LuxR | Aliivibrio fischeri | IC50 | 40.0000 | 1 | 1 |
| Tyrosine-protein kinase Fyn | Homo sapiens (human) | IC50 | 1.1950 | 1 | 1 |
| Tyrosine-protein kinase Lck | Homo sapiens (human) | IC50 | 8.0330 | 1 | 1 |
| ubiquitin-conjugating enzyme E2 N | Homo sapiens (human) | IC50 | 20.0000 | 1 | 2 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Homo sapiens (human) | Kd | 0.0010 | 1 | 1 |
| 7-dehydrocholesterol reductase | Homo sapiens (human) | Kd | 0.0010 | 1 | 1 |
| Angiotensin-converting enzyme 2 | Homo sapiens (human) | EC50 | 51.4950 | 1 | 2 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | EC50 | 56.5000 | 1 | 1 |
| Estrogen receptor | Homo sapiens (human) | EC50 | 0.7233 | 6 | 8 |
| Estrogen receptor | Rattus norvegicus (Norway rat) | EC50 | 150.0000 | 1 | 2 |
| Estrogen receptor | Homo sapiens (human) | Kd | 0.0047 | 1 | 1 |
| Estrogen receptor beta | Homo sapiens (human) | EC50 | 0.9808 | 3 | 5 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | EC50 | 150.0000 | 1 | 2 |
| Estrogen-related receptor gamma | Homo sapiens (human) | EC50 | 0.0150 | 1 | 1 |
| Lysosomal acid glucosylceramidase | Homo sapiens (human) | EC50 | 2.5000 | 1 | 1 |
| Nuclear receptor subfamily 1 group I member 2 | Homo sapiens (human) | EC50 | 5.2750 | 1 | 2 |
| Procathepsin L | Homo sapiens (human) | EC50 | 51.4950 | 1 | 2 |
| Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | EC50 | 51.4950 | 1 | 2 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | EC50 | 51.4950 | 1 | 2 |
| Replicase polyprotein 1ab | Human coronavirus 229E | EC50 | 51.4950 | 1 | 2 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | EC50 | 51.4950 | 1 | 2 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | EC50 | 51.4950 | 1 | 2 |
| Spike glycoprotein | Betacoronavirus England 1 | EC50 | 51.4950 | 1 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | EC50 | 51.4950 | 1 | 2 |
| streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 | 78.0860 | 2 | 2 |
| Transient receptor potential cation channel subfamily A member 1 | Homo sapiens (human) | EC50 | 0.4900 | 1 | 1 |
| Transmembrane protease serine 2 | Homo sapiens (human) | EC50 | 51.4950 | 1 | 2 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Estrogen receptor | Rattus norvegicus (Norway rat) | A50 | 0.0200 | 1 | 1 |
| Estrogen receptor | Homo sapiens (human) | Activity | 0.0001 | 1 | 1 |
| Estrogen receptor | Homo sapiens (human) | DC50 | 0.0304 | 1 | 3 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | A50 | 0.0200 | 1 | 1 |
| Glutathione reductase, mitochondrial | Homo sapiens (human) | Km | 160.0000 | 1 | 1 |
| heat shock protein 90, putative | Plasmodium falciparum 3D7 | AC50 | 7.7570 | 1 | 1 |
| heat shock protein HSP 90-alpha isoform 2 | Homo sapiens (human) | AC50 | 6.3200 | 1 | 1 |
| interferon gamma precursor | Homo sapiens (human) | AC50 | 35.2400 | 1 | 1 |
| UDP-glucuronosyltransferase 1A4 | Homo sapiens (human) | Km | 32.0000 | 1 | 1 |