A compound which inhibits or antagonises the biosynthesis or actions of estrogens.
ChEBI ID: 50837
| Member | Definition | Class |
|---|---|---|
| clomiphene | clomiphene | |
| danazol | danazol | |
| fulvestrant | A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group.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 |
| raloxifene | A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively. | raloxifene |
| raloxifene hydrochloride | A hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride. | raloxifene hydrochloride |
| tamoxifen | tamoxifen | |
| toremifene | toremifene |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 3,388 (13.07) | 18.7374 |
| 1990's | 5,299 (20.44) | 18.2507 |
| 2000's | 8,200 (31.64) | 29.6817 |
| 2010's | 7,154 (27.60) | 24.3611 |
| 2020's | 1,878 (7.25) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 3,312 (11.30%) | 5.53% |
| Reviews | 4,062 (13.85%) | 6.00% |
| Case Studies | 1,943 (6.63%) | 4.05% |
| Observational | 88 (0.30%) | 0.25% |
| Other | 19,913 (67.92%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 29.8816 | 1 | 2 |
| 67.9K protein | Vaccinia virus | Potency | 8.9125 | 1 | 1 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 22.2288 | 4 | 16 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 42.7369 | 2 | 8 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 1.9974 | 2 | 4 |
| Alpha-synuclein | Homo sapiens (human) | Potency | 18.3564 | 1 | 1 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 35.4813 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 26.0249 | 11 | 55 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 47.8957 | 2 | 3 |
| arylsulfatase A | Homo sapiens (human) | Potency | 5.0669 | 1 | 2 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 11.8292 | 1 | 2 |
| Ataxin-2 | Homo sapiens (human) | Potency | 49.7012 | 2 | 8 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 33.8078 | 1 | 1 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 59.7588 | 2 | 7 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 56.2341 | 2 | 2 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 56.4631 | 1 | 4 |
| caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 51.9755 | 1 | 3 |
| caspase-3 | Homo sapiens (human) | Potency | 56.4631 | 1 | 4 |
| Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 51.9755 | 1 | 3 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 58.5372 | 3 | 14 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 24.8808 | 2 | 6 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 5.0119 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 23.5079 | 2 | 3 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 6.8184 | 1 | 3 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 50.4512 | 1 | 2 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 40.0831 | 1 | 5 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 6.8184 | 1 | 3 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 35.6383 | 2 | 3 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 8.1548 | 1 | 2 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 12.5674 | 1 | 2 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 1.4364 | 1 | 3 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 10.3604 | 1 | 2 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 21.5617 | 1 | 3 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 9.4764 | 2 | 8 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 2.3057 | 2 | 4 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 6.9110 | 1 | 9 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 4.0904 | 2 | 3 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 18.9850 | 1 | 2 |
| Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | Potency | 5.0119 | 1 | 1 |
| DNA dC->dU-editing enzyme APOBEC-3G isoform 1 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| DNA polymerase III, partial | Bacillus subtilis | Potency | 29.9349 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 7.7690 | 1 | 2 |
| endonuclease IV | Escherichia coli | Potency | 19.9526 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 12.6339 | 12 | 79 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 28.5520 | 3 | 19 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 29.8799 | 9 | 56 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 15.7857 | 1 | 9 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 16.2294 | 4 | 8 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 38.6146 | 5 | 12 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 35.4813 | 1 | 2 |
| G | Vesicular stomatitis virus | Potency | 1.4364 | 1 | 3 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| GALC protein | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| geminin | Homo sapiens (human) | Potency | 17.9646 | 3 | 8 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 8.3960 | 2 | 19 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 15.1861 | 1 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 17.2206 | 1 | 2 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 22.7571 | 1 | 4 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 35.0866 | 5 | 23 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 6.3227 | 1 | 10 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 52.8902 | 2 | 9 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 10.0535 | 2 | 12 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 62.2287 | 2 | 5 |
| histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 1.4364 | 1 | 3 |
| huntingtin isoform 2 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 51.6654 | 2 | 10 |
| IDH1 | Homo sapiens (human) | Potency | 17.3582 | 1 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 1.4364 | 1 | 6 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 22.4748 | 1 | 3 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 22.4748 | 1 | 3 |
| Interferon beta | Homo sapiens (human) | Potency | 15.4436 | 3 | 10 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 11.3715 | 2 | 4 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 13.8834 | 1 | 4 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 26.2769 | 1 | 3 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 10.3008 | 2 | 6 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 2 | 2 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 35.4813 | 1 | 1 |
| NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 58.0479 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 34.8718 | 4 | 15 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 16.3601 | 1 | 1 |
| nuclear factor NF-kappa-B p105 subunit isoform 1 | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 43.0632 | 2 | 8 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 23.5433 | 2 | 4 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 18.0636 | 1 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 52.7793 | 3 | 15 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 89.1251 | 1 | 2 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 79.4328 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 20.4276 | 2 | 4 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 37.9330 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 40.4041 | 5 | 15 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 33.1519 | 4 | 15 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 52.8827 | 2 | 6 |
| polyprotein | Zika virus | Potency | 35.4813 | 1 | 2 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 7.5397 | 1 | 3 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 12.5893 | 1 | 2 |
| PPM1D protein | Homo sapiens (human) | Potency | 24.3226 | 1 | 4 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 18.1366 | 3 | 13 |
| pregnane X receptor | Rattus norvegicus (Norway rat) | Potency | 46.7791 | 1 | 2 |
| progesterone receptor | Homo sapiens (human) | Potency | 25.9540 | 3 | 17 |
| Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 17.1689 | 2 | 20 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 91.9997 | 1 | 1 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 11.0180 | 1 | 2 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 41.3709 | 3 | 18 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 22.9981 | 4 | 15 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 19.7263 | 4 | 7 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 43.3619 | 3 | 10 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 43.3619 | 3 | 10 |
| Smad3 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 34.8462 | 1 | 4 |
| TDP1 protein | Homo sapiens (human) | Potency | 22.7986 | 2 | 10 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 34.2650 | 3 | 4 |
| Thrombopoietin | Homo sapiens (human) | Potency | 15.8489 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 10.5717 | 3 | 21 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 39.1512 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 40.8103 | 6 | 11 |
| thyrotropin-releasing hormone receptor | Homo sapiens (human) | Potency | 27.3185 | 2 | 4 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| ubiquitin carboxyl-terminal hydrolase 2 isoform a | Homo sapiens (human) | Potency | 5.0119 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 48.6554 | 1 | 4 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 33.4156 | 2 | 9 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 27.9491 | 4 | 16 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 46.4852 | 1 | 3 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 6.3227 | 1 | 10 |
| 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 | 0.0030 | 1 | 2 |
| 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 | 5.0337 | 1 | 3 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 1.4380 | 1 | 3 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | IC50 | 1.2195 | 1 | 2 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 0.5403 | 2 | 3 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 | 0.8190 | 1 | 2 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 0.4290 | 1 | 2 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | IC50 | 0.8190 | 1 | 2 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | Ki | 0.4290 | 1 | 2 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | IC50 | 2.6790 | 1 | 1 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | Ki | 1.8232 | 2 | 5 |
| 7-dehydrocholesterol reductase | Homo sapiens (human) | IC50 | 0.0120 | 1 | 1 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 0.4000 | 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 | 4.6050 | 1 | 2 |
| Adenosine receptor A2a | Homo sapiens (human) | Ki | 2.5850 | 1 | 2 |
| Adenosine receptor A3 | Homo sapiens (human) | IC50 | 7.4305 | 1 | 2 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 4.2005 | 1 | 2 |
| Aldehyde oxidase | Homo sapiens (human) | IC50 | 0.0055 | 2 | 2 |
| Aldehyde oxidase | Homo sapiens (human) | Ki | 0.0009 | 4 | 4 |
| Aldehyde oxidase 1 | Macaca fascicularis (crab-eating macaque) | IC50 | 0.5000 | 1 | 1 |
| Aldehyde oxidase 1 | Mus musculus (house mouse) | IC50 | 0.5000 | 1 | 1 |
| Aldehyde oxidase 1 | Oryctolagus cuniculus (rabbit) | IC50 | 0.0080 | 1 | 1 |
| Aldehyde oxidase 1 | Rattus norvegicus (Norway rat) | IC50 | 1.1000 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | IC50 | 2.4840 | 1 | 3 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 2.4633 | 1 | 3 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 7.4305 | 1 | 2 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 4.2005 | 1 | 2 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 7.4305 | 1 | 2 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 4.2005 | 1 | 2 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | IC50 | 2.9775 | 1 | 2 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Ki | 1.4635 | 1 | 2 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 | 7.3090 | 1 | 3 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 2.7410 | 1 | 3 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | IC50 | 10.1263 | 1 | 3 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 4.6227 | 1 | 3 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | IC50 | 12.2450 | 1 | 2 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 1.7790 | 1 | 2 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| Androgen receptor | Rattus norvegicus (Norway rat) | IC50 | 12.0466 | 2 | 4 |
| Androgen receptor | Rattus norvegicus (Norway rat) | Ki | 7.5580 | 1 | 2 |
| Angiotensin-converting enzyme | Oryctolagus cuniculus (rabbit) | IC50 | 0.9670 | 1 | 1 |
| Angiotensin-converting enzyme | Oryctolagus cuniculus (rabbit) | Ki | 0.7922 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 4 |
| 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 | 12.3615 | 1 | 2 |
| Beta-3 adrenergic receptor | Homo sapiens (human) | Ki | 9.2715 | 1 | 2 |
| 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 | 6.1750 | 1 | 2 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 58.1909 | 6 | 11 |
| C-8 sterol isomerase | Saccharomyces cerevisiae S288C | Ki | 0.7830 | 1 | 2 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 4 |
| Chain A, CES1 protein | Homo sapiens (human) | Ki | 15.2000 | 1 | 1 |
| Cruzipain | Trypanosoma cruzi | IC50 | 73.6667 | 3 | 3 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 0.0190 | 1 | 1 |
| Cytochrome P450 2B6 | Homo sapiens (human) | Ki | 0.9000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 1.1500 | 1 | 2 |
| Cytochrome P450 2J2 | Homo sapiens (human) | IC50 | 0.0318 | 3 | 4 |
| Cytochrome P450 2J2 | Homo sapiens (human) | Ki | 0.0200 | 1 | 2 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 5.0500 | 2 | 2 |
| D(1A) dopamine receptor | Homo sapiens (human) | IC50 | 10.9383 | 1 | 3 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 5.4693 | 1 | 3 |
| D(2) dopamine receptor | Homo sapiens (human) | IC50 | 7.5295 | 1 | 2 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 2.5095 | 1 | 2 |
| D(3) dopamine receptor | Homo sapiens (human) | IC50 | 10.4990 | 1 | 3 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 3.5650 | 1 | 3 |
| 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 | 9.9915 | 1 | 2 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 3.5220 | 1 | 2 |
| 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 | 0.5311 | 113 | 129 |
| Estrogen receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0039 | 4 | 4 |
| Estrogen receptor | Homo sapiens (human) | Ki | 0.2963 | 15 | 18 |
| Estrogen receptor | Rattus norvegicus (Norway rat) | Ki | 0.0004 | 1 | 1 |
| Estrogen receptor beta | Homo sapiens (human) | IC50 | 0.5188 | 72 | 81 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | IC50 | 0.1584 | 3 | 3 |
| Estrogen receptor beta | Homo sapiens (human) | Ki | 0.0177 | 12 | 15 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | Ki | 0.0027 | 1 | 1 |
| Estrogen-related receptor gamma | Homo sapiens (human) | IC50 | 0.0622 | 1 | 1 |
| Gastric inhibitory polypeptide receptor | Homo sapiens (human) | IC50 | 0.0004 | 1 | 1 |
| Glucocorticoid receptor | Homo sapiens (human) | IC50 | 4.3140 | 1 | 1 |
| Glucocorticoid receptor | Homo sapiens (human) | Ki | 1.9610 | 1 | 1 |
| Glycine receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | IC50 | 4.3140 | 1 | 1 |
| Glycine receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Ki | 1.9610 | 1 | 1 |
| Glycine receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | IC50 | 4.3140 | 1 | 1 |
| Glycine receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Ki | 1.9610 | 1 | 1 |
| Glycine receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | IC50 | 4.3140 | 1 | 1 |
| Glycine receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Ki | 1.9610 | 1 | 1 |
| Glycine receptor subunit beta | Rattus norvegicus (Norway rat) | IC50 | 4.3140 | 1 | 1 |
| Glycine receptor subunit beta | Rattus norvegicus (Norway rat) | Ki | 1.9610 | 1 | 1 |
| 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 | 10.9163 | 1 | 3 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 4.3667 | 1 | 3 |
| Lysine-specific histone demethylase 1A | Homo sapiens (human) | IC50 | 2.0800 | 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 | 10.9497 | 1 | 3 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 4.4447 | 1 | 3 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 4 |
| 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 | 10.3605 | 1 | 2 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 2.1960 | 1 | 2 |
| 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 | 9.0556 | 7 | 9 |
| Phospholipase D1 | Rattus norvegicus (Norway rat) | IC50 | 20.0000 | 1 | 2 |
| Phospholipase D2 | Homo sapiens (human) | IC50 | 7.6000 | 3 | 4 |
| Platelet-activating factor acetylhydrolase | Homo sapiens (human) | IC50 | 0.3015 | 2 | 3 |
| Polyunsaturated fatty acid 5-lipoxygenase | Homo sapiens (human) | Ki | 0.0298 | 3 | 6 |
| 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 | 40.0458 | 3 | 5 |
| 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 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 3.5800 | 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 | 0.3510 | 1 | 2 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 0.0919 | 2 | 4 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | IC50 | 3.5173 | 1 | 3 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 2.7943 | 1 | 3 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 | 2.4840 | 1 | 3 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 2.4633 | 1 | 3 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | IC50 | 7.1100 | 1 | 3 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 3.7777 | 1 | 3 |
| Steroid hormone receptor ERR1 | Homo sapiens (human) | IC50 | 0.1010 | 1 | 2 |
| Substance-K receptor | Homo sapiens (human) | IC50 | 11.4130 | 1 | 3 |
| Substance-K receptor | Homo sapiens (human) | Ki | 3.8043 | 1 | 3 |
| 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 | 2.4305 | 1 | 2 |
| Tyrosine-protein kinase Lck | Homo sapiens (human) | IC50 | 8.0330 | 1 | 1 |
| ubiquitin-conjugating enzyme E2 N | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| 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 | 31.9650 | 1 | 4 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | EC50 | 56.5000 | 1 | 1 |
| Complement C5 | Homo sapiens (human) | Kd | 0.7100 | 1 | 1 |
| Envelope glycoprotein | Ebola virus - Mayinga, Zaire, 1976 | EC50 | 0.0628 | 2 | 2 |
| Envelope glycoprotein | Ebola virus - Mayinga, Zaire, 1976 | Kd | 16.0000 | 2 | 2 |
| Estrogen receptor | Homo sapiens (human) | EC50 | 0.5301 | 8 | 11 |
| 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 | 0.8607 | 4 | 6 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | EC50 | 150.0000 | 1 | 2 |
| HLA class I histocompatibility antigen, A alpha chain | Homo sapiens (human) | Kd | 22.0000 | 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 | 6.8300 | 1 | 2 |
| Phospholipase D1 | Homo sapiens (human) | EC50 | 9.2500 | 2 | 2 |
| Procathepsin L | Homo sapiens (human) | EC50 | 31.9650 | 1 | 4 |
| Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | EC50 | 31.9650 | 1 | 4 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | EC50 | 31.9650 | 1 | 4 |
| Replicase polyprotein 1ab | Human coronavirus 229E | EC50 | 31.9650 | 1 | 4 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | EC50 | 31.9650 | 1 | 4 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | EC50 | 31.9650 | 1 | 4 |
| Sex hormone-binding globulin | Homo sapiens (human) | Kd | 0.0063 | 1 | 1 |
| Spike glycoprotein | Betacoronavirus England 1 | EC50 | 31.9650 | 1 | 4 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | EC50 | 31.9650 | 1 | 4 |
| streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 | 78.0860 | 2 | 2 |
| Transmembrane protease serine 2 | Homo sapiens (human) | EC50 | 31.9650 | 1 | 4 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Aldehyde oxidase | Homo sapiens (human) | Kii | 0.0070 | 1 | 1 |
| 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 | 0.0456 | 1 | 2 |
| Estrogen receptor | Homo sapiens (human) | Ka | 0.0002 | 1 | 1 |
| Estrogen receptor | Homo sapiens (human) | Relative binding affinity | 0.0180 | 1 | 1 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | A50 | 0.0200 | 1 | 1 |
| Estrogen receptor beta | Homo sapiens (human) | Ka | 0.0412 | 1 | 1 |
| Estrogen receptor beta | Homo sapiens (human) | Relative binding affinity | 0.0040 | 1 | 1 |
| interferon gamma precursor | Homo sapiens (human) | AC50 | 35.2400 | 1 | 1 |
| Prolyl 4-hydroxylase, beta polypeptide | Homo sapiens (human) | AC50 | 45.2600 | 1 | 1 |
| UDP-glucuronosyltransferase 1A4 | Homo sapiens (human) | Km | 32.0000 | 1 | 1 |