A substance that possess antiestrogenic actions but can also produce estrogenic effects as well. It acts as complete or partial agonist or as antagonist. It can be either steroidal or nonsteroidal in structure.
ChEBI ID: 50739
| Member | Definition | Class |
|---|---|---|
| chlorotrianisene | chlorotrianisene | |
| clomiphene | clomiphene | |
| ethynodiol diacetate | ethynodiol diacetate | |
| ly 117018 | A member of the class of 1-benzothiophenes that is raloxifene in which the piperidin-1-yl group has been replaced by a pyrrolidin-1-yl group.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 |
| ospemifene | An organochlorine compound that is a selective estrogen receptor modulator; used for treatment of dyspareunia. | ospemifene |
| 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member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively.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 | 3,137 (13.95) | 18.7374 |
| 1990's | 4,574 (20.34) | 18.2507 |
| 2000's | 7,072 (31.45) | 29.6817 |
| 2010's | 6,160 (27.40) | 24.3611 |
| 2020's | 1,542 (6.86) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 2,910 (11.54%) | 5.53% |
| Reviews | 3,536 (14.03%) | 6.00% |
| Case Studies | 1,395 (5.53%) | 4.05% |
| Observational | 77 (0.31%) | 0.25% |
| Other | 17,294 (68.59%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| 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 | 43.3530 | 2 | 9 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 7.2347 | 2 | 5 |
| 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 | 28.2534 | 10 | 58 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 66.6968 | 2 | 4 |
| arylsulfatase A | Homo sapiens (human) | Potency | 5.3582 | 1 | 1 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 16.3535 | 1 | 1 |
| Ataxin-2 | Homo sapiens (human) | Potency | 48.0685 | 2 | 7 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 33.8078 | 1 | 1 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 59.5302 | 2 | 6 |
| 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 | 54.7222 | 3 | 16 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 24.8808 | 2 | 6 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 29.3157 | 1 | 3 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 5.0119 | 1 | 1 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 16.0599 | 1 | 4 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 20.4443 | 2 | 5 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 15.0665 | 2 | 4 |
| 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 | 15.0665 | 2 | 4 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 40.7872 | 2 | 4 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 5.4699 | 1 | 3 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 12.5674 | 1 | 2 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 6.4485 | 1 | 3 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 6.9178 | 1 | 1 |
| 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 | 1.8306 | 2 | 3 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 4.6023 | 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 | 12.5167 | 12 | 87 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 17.5124 | 3 | 16 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 37.8276 | 9 | 50 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 17.6752 | 1 | 8 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 16.2294 | 4 | 8 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 38.4210 | 5 | 10 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 35.4813 | 1 | 2 |
| G | Vesicular stomatitis virus | Potency | 6.4485 | 1 | 3 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 9.4764 | 1 | 4 |
| 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 | 17.7910 | 3 | 10 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 10.9533 | 2 | 12 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 11.2947 | 1 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 2.8184 | 1 | 1 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 22.7571 | 1 | 4 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 34.5228 | 5 | 22 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 5.0113 | 1 | 9 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 53.8118 | 2 | 6 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 10.0535 | 2 | 12 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 46.0876 | 2 | 4 |
| 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 | 6.4485 | 1 | 3 |
| huntingtin isoform 2 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 51.9855 | 2 | 10 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 10.0000 | 2 | 2 |
| IDH1 | Homo sapiens (human) | Potency | 17.3582 | 1 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 6.4485 | 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 | 19.8575 | 3 | 10 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 9.1536 | 2 | 5 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 16.1305 | 1 | 5 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 26.2769 | 1 | 3 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 9.6326 | 2 | 7 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 2 | 2 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 11.8961 | 1 | 2 |
| 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 | 37.5298 | 4 | 12 |
| 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 | 41.8317 | 2 | 11 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 18.8336 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 22.0044 | 2 | 5 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 59.8630 | 3 | 12 |
| 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 | 21.4721 | 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 | 43.0564 | 5 | 13 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 36.9961 | 4 | 10 |
| 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 | 20.1075 | 3 | 10 |
| pregnane X receptor | Rattus norvegicus (Norway rat) | Potency | 62.0506 | 1 | 2 |
| progesterone receptor | Homo sapiens (human) | Potency | 34.4391 | 3 | 14 |
| Rap guanine nucleotide exchange factor 4 | Homo sapiens (human) | Potency | 4.4668 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 24.8643 | 2 | 17 |
| 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 | 39.5782 | 3 | 17 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 24.8291 | 4 | 13 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 19.7263 | 4 | 7 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 42.7392 | 3 | 9 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 42.7392 | 3 | 9 |
| Smad3 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 30.1210 | 1 | 5 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 11.9048 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 23.1090 | 2 | 13 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 55.1587 | 1 | 2 |
| Thrombopoietin | Homo sapiens (human) | Potency | 15.8489 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 13.3712 | 3 | 23 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 39.1512 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 35.6395 | 5 | 16 |
| 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 | 45.7952 | 1 | 6 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 37.2901 | 2 | 12 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 26.5734 | 4 | 10 |
| 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 | 5.0113 | 1 | 9 |
| 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 | 3.1255 | 1 | 2 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 0.8930 | 1 | 2 |
| 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 | 3.7010 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 2.0920 | 1 | 1 |
| 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 | 0.8770 | 1 | 2 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 0.8695 | 1 | 2 |
| 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 | 2.9775 | 1 | 2 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Ki | 1.4635 | 1 | 2 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 | 1.7995 | 1 | 2 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 0.6750 | 1 | 2 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | IC50 | 3.6080 | 1 | 2 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 1.6470 | 1 | 2 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | IC50 | 0.7380 | 1 | 1 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 0.1070 | 1 | 1 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | IC50 | 102.1450 | 2 | 2 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| Androgen receptor | Rattus norvegicus (Norway rat) | IC50 | 12.8186 | 2 | 4 |
| Androgen receptor | Rattus norvegicus (Norway rat) | Ki | 8.5875 | 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 | 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 |
| Bile acid receptor | Homo sapiens (human) | IC50 | 11.5600 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 65.2125 | 6 | 8 |
| 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 | 2 |
| Chain A, CES1 protein | Homo sapiens (human) | Ki | 15.2000 | 1 | 1 |
| Cruzipain | Trypanosoma cruzi | IC50 | 73.6667 | 3 | 3 |
| Cytochrome P450 2B6 | Homo sapiens (human) | Ki | 0.9000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 5.0500 | 2 | 2 |
| D(1A) dopamine receptor | Homo sapiens (human) | IC50 | 6.1830 | 1 | 2 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 3.0915 | 1 | 2 |
| 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 | 1.3185 | 1 | 2 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 0.4475 | 1 | 2 |
| 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 | 0.5169 | 90 | 98 |
| Estrogen receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0032 | 3 | 3 |
| Estrogen receptor | Homo sapiens (human) | Ki | 0.0173 | 13 | 14 |
| Estrogen receptor | Rattus norvegicus (Norway rat) | Ki | 0.0004 | 1 | 1 |
| Estrogen receptor beta | Homo sapiens (human) | IC50 | 0.5919 | 63 | 71 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | IC50 | 0.1584 | 3 | 3 |
| Estrogen receptor beta | Homo sapiens (human) | Ki | 0.0213 | 10 | 12 |
| 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 |
| 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 | 8.6155 | 1 | 2 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 3.4465 | 1 | 2 |
| 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 | 9.3850 | 1 | 2 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 3.8095 | 1 | 2 |
| 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 |
| 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 | 0.0844 | 2 | 2 |
| 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 | 33.4096 | 3 | 3 |
| 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 | 1.8550 | 1 | 2 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 1.4735 | 1 | 2 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 | 0.8770 | 1 | 2 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 0.8695 | 1 | 2 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | IC50 | 2.9550 | 1 | 2 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 1.5700 | 1 | 2 |
| Steroid hormone receptor ERR1 | Homo sapiens (human) | IC50 | 0.2000 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | IC50 | 3.8295 | 1 | 2 |
| Substance-K receptor | Homo sapiens (human) | Ki | 1.2765 | 1 | 2 |
| 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 | 0.7286 | 6 | 8 |
| Estrogen receptor | Rattus norvegicus (Norway rat) | EC50 | 150.0000 | 1 | 2 |
| 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 | 11.7100 | 1 | 1 |
| 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 |
| 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) | DC50 | 0.0910 | 1 | 1 |
| 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 |