Page last updated: 2024-08-05 15:34:49
anti-estrogen
A drug which acts to reduce estrogenic activity in the body, either by reducing the amount of estrogen or by reducing the activity of whatever estrogen is present.
ChEBI ID: 50751
Members (8)
| Member | Definition | Class |
|---|---|---|
| 9,9-bis(4-hydroxyphenyl)fluorene | A member of the class of fluorenes that is 9H-fluorene in which both of the hydrogens at position 9 have been replaced by p-hydroxyphenyl groups. | 9,9-bis(4-hydroxyphenyl)fluorene |
| danazol | danazol | |
| 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 |
| leuprolide | An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-leucyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant (particularly as the acetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty. | leuprolide |
| monopentyl phthalate | A phthalic acid monoester obtained by formal condensation of one of the carboxy groups of phthalic acid with the hydroxy group of pentanol. | monopentyl phthalate |
| nafarelin | An oligopeptide comprising of 5-oxo-L-proline, L-histidine, L-tryptophan, L-serine, L-tyrosine, 3-(2-naphthyl)-D-alanine, L-leucine, L-arginine and L-prolylglycinamide residues joined sequence by peptide linkages. It is a gonadotropin releasing hormone agonist that is used to treat central precocious puberty in children and endometriosis in women. | nafarelin |
| ru 58668 | A 17beta-hydroxy steroid that is 17beta-estradiol in the the hydrogen at the 11beta position has been replaced by a p-({5-[(4,4,5,5,5-pentafluoropentyl)sulfonyl]pentyl}oxy)phenyl group.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 n-oxide | A tertiary amine oxide resulting from the formal oxidation of the amino group of tamoxifen. | tamoxifen N-oxide |
Research
Studies (5,612)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 1,171 (20.87) | 18.7374 |
| 1990's | 1,882 (33.54) | 18.2507 |
| 2000's | 1,364 (24.31) | 29.6817 |
| 2010's | 954 (17.00) | 24.3611 |
| 2020's | 241 (4.29) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1,159 (18.95%) | 5.53% |
| Reviews | 691 (11.30%) | 6.00% |
| Case Studies | 1,031 (16.86%) | 4.05% |
| Observational | 19 (0.31%) | 0.25% |
| Other | 3,215 (52.58%) | 84.16% |
Protein Targets (94)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| acetylcholinesterase | Homo sapiens (human) | Potency | 64.6366 | 2 | 2 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 54.9410 | 2 | 2 |
| AR protein | Homo sapiens (human) | Potency | 16.6853 | 11 | 26 |
| Ataxin-2 | Homo sapiens (human) | Potency | 61.1306 | 1 | 1 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 61.1306 | 1 | 1 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 68.5896 | 1 | 1 |
| caspase-3 | Homo sapiens (human) | Potency | 68.5896 | 1 | 1 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 63.6762 | 3 | 5 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 5.6234 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 1.3803 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 13.8029 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 3.4671 | 1 | 1 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 42.3375 | 1 | 3 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 25.7889 | 11 | 26 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 48.8057 | 2 | 6 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 38.7979 | 6 | 18 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 34.9069 | 4 | 7 |
| G | Vesicular stomatitis virus | Potency | 1.3803 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 14.3299 | 1 | 3 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 14.9557 | 2 | 6 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 17.7828 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 45.5963 | 4 | 8 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 18.6903 | 1 | 3 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 42.7007 | 2 | 4 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 97.0527 | 2 | 2 |
| 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 | 55.7549 | 2 | 4 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 1.3803 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 2.7859 | 2 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 36.0358 | 3 | 7 |
| nuclear factor NF-kappa-B p105 subunit isoform 1 | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 54.9410 | 2 | 2 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 27.6303 | 3 | 5 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 89.1251 | 1 | 2 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 16.1366 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 45.6169 | 4 | 7 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 37.2414 | 4 | 8 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 35.9222 | 2 | 5 |
| pregnane X receptor | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 15.0158 | 3 | 8 |
| Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 34.8931 | 2 | 6 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 42.9539 | 3 | 9 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 33.0584 | 3 | 7 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 48.9662 | 1 | 1 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 48.9662 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 33.4983 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 20.4996 | 3 | 7 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 42.2090 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 28.2707 | 2 | 6 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 33.5562 | 2 | 3 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 31.1773 | 4 | 8 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 18.6903 | 1 | 3 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | IC50 | 8.8500 | 1 | 1 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 2.5280 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | IC50 | 11.1600 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 6.3090 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | IC50 | 5.6980 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 5.6510 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 11.1600 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 6.3090 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 11.1600 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 6.3090 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 | 18.3280 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 6.8730 | 1 | 1 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | IC50 | 23.1630 | 1 | 1 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 10.5740 | 1 | 1 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | IC50 | 23.7520 | 1 | 1 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 3.4510 | 1 | 1 |
| Androgen receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0120 | 1 | 1 |
| Androgen receptor | Rattus norvegicus (Norway rat) | Ki | 0.0080 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Beta-3 adrenergic receptor | Homo sapiens (human) | IC50 | 17.0200 | 1 | 1 |
| Beta-3 adrenergic receptor | Homo sapiens (human) | Ki | 12.7650 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 15.8000 | 3 | 3 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 0.0190 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
| Cytochrome P450 2J2 | Homo sapiens (human) | IC50 | 0.0318 | 3 | 4 |
| Cytochrome P450 2J2 | Homo sapiens (human) | Ki | 0.0200 | 1 | 2 |
| D(1A) dopamine receptor | Homo sapiens (human) | IC50 | 20.4490 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 10.2250 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | IC50 | 28.8600 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 9.8000 | 1 | 1 |
| Estrogen receptor | Homo sapiens (human) | IC50 | 4.5450 | 4 | 4 |
| Estrogen receptor | Homo sapiens (human) | Ki | 1.2729 | 4 | 4 |
| Estrogen receptor beta | Homo sapiens (human) | Ki | 0.0029 | 3 | 3 |
| 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 |
| Gonadotropin-releasing hormone receptor | Homo sapiens (human) | IC50 | 0.0005 | 3 | 3 |
| Gonadotropin-releasing hormone receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0006 | 3 | 3 |
| Gonadotropin-releasing hormone receptor | Rattus norvegicus (Norway rat) | Ki | 5,370,320,000,000,000.0000 | 1 | 1 |
| Kappa-type opioid receptor | Homo sapiens (human) | IC50 | 15.5180 | 1 | 1 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 6.2070 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | IC50 | 14.0790 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 5.7150 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | IC50 | 17.7470 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 3.7620 | 1 | 1 |
| Polyunsaturated fatty acid 5-lipoxygenase | Homo sapiens (human) | Ki | 0.0046 | 1 | 1 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | IC50 | 6.8420 | 1 | 1 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 5.4360 | 1 | 1 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 | 5.6980 | 1 | 1 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 5.6510 | 1 | 1 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | IC50 | 15.4200 | 1 | 1 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 8.1930 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | IC50 | 26.5800 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | Ki | 8.8600 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Sex hormone-binding globulin | Homo sapiens (human) | Kd | 0.0063 | 1 | 1 |