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)

MemberDefinitionClass
9,9-bis(4-hydroxyphenyl)fluoreneA member of the class of fluorenes that is 9H-fluorene in which both of the hydrogens at position 9 have been replaced by p-hydroxyphenyl groups.9,9-bis(4-hydroxyphenyl)fluorene
danazoldanazol
ici 164384A 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
leuprolideAn 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 phthalateA phthalic acid monoester obtained by formal condensation of one of the carboxy groups of phthalic acid with the hydroxy group of pentanol.monopentyl phthalate
nafarelinAn 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ru 58668A 17beta-hydroxy steroid that is 17beta-estradiol in the the hydrogen at the 11beta position has been replaced by a p-({5-[(4,4,5,5,5-pentafluoropentyl)sulfonyl]pentyl}oxy)phenyl group.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-oxideA tertiary amine oxide resulting from the formal oxidation of the amino group of tamoxifen.tamoxifen N-oxide

Research

Studies (5,612)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19901,171 (20.87)18.7374
1990's1,882 (33.54)18.2507
2000's1,364 (24.31)29.6817
2010's954 (17.00)24.3611
2020's241 (4.29)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,159 (18.95%)5.53%
Reviews691 (11.30%)6.00%
Case Studies1,031 (16.86%)4.05%
Observational19 (0.31%)0.25%
Other3,215 (52.58%)84.16%

Protein Targets (94)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
acetylcholinesteraseHomo sapiens (human)Potency64.636622
activating transcription factor 6Homo sapiens (human)Potency54.941022
AR proteinHomo sapiens (human)Potency16.68531126
Ataxin-2Homo sapiens (human)Potency61.130611
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency61.130611
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency68.589611
caspase-3Homo sapiens (human)Potency68.589611
Cellular tumor antigen p53Homo sapiens (human)Potency63.676235
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency5.623411
cytochrome P450 2C9, partialHomo sapiens (human)Potency1.380311
cytochrome P450 2D6Homo sapiens (human)Potency13.802911
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency3.467111
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency42.337513
estrogen nuclear receptor alphaHomo sapiens (human)Potency25.78891126
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency48.805726
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency38.7979618
farnesoid X nuclear receptorHomo sapiens (human)Potency34.906947
GVesicular stomatitis virusPotency1.380311
gemininHomo sapiens (human)Potency14.329913
GLI family zinc finger 3Homo sapiens (human)Potency14.955726
glp-1 receptor, partialHomo sapiens (human)Potency17.782811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency45.596348
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency18.690313
Guanine nucleotide-binding protein GHomo sapiens (human)Potency11.220211
heat shock protein beta-1Homo sapiens (human)Potency42.700724
Histone H2A.xCricetulus griseus (Chinese hamster)Potency97.052722
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency1.380311
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency55.754924
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency1.380312
Interferon betaHomo sapiens (human)Potency2.785922
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency36.035837
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency50.118711
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency54.941022
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency7.943311
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency27.630335
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency89.125112
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency16.136611
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency45.616947
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency37.241448
pregnane X nuclear receptorHomo sapiens (human)Potency35.922225
pregnane X receptorRattus norvegicus (Norway rat)Potency14.125411
progesterone receptorHomo sapiens (human)Potency15.015838
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency3.162311
RAR-related orphan receptor gammaMus musculus (house mouse)Potency34.893126
regulator of G-protein signaling 4Homo sapiens (human)Potency44.668411
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency42.953939
retinoid X nuclear receptor alphaHomo sapiens (human)Potency33.058437
SMAD family member 2Homo sapiens (human)Potency48.966211
SMAD family member 3Homo sapiens (human)Potency48.966211
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
TDP1 proteinHomo sapiens (human)Potency33.498322
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency20.499637
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency42.209022
thyroid stimulating hormone receptorHomo sapiens (human)Potency28.270726
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency33.556223
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency31.177348
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency18.690313

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC508.850011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki2.528011
Adenosine receptor A3Homo sapiens (human)IC5011.160011
Adenosine receptor A3Homo sapiens (human)Ki6.309011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC505.698011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki5.651011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC5011.160011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki6.309011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC5011.160011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki6.309011
Alpha-2A adrenergic receptorHomo sapiens (human)IC5018.328011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki6.873011
Alpha-2B adrenergic receptorHomo sapiens (human)IC5023.163011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki10.574011
Alpha-2C adrenergic receptorHomo sapiens (human)IC5023.752011
Alpha-2C adrenergic receptorHomo sapiens (human)Ki3.451011
Androgen receptorRattus norvegicus (Norway rat)IC500.012011
Androgen receptorRattus norvegicus (Norway rat)Ki0.008011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
Beta-3 adrenergic receptorHomo sapiens (human)IC5017.020011
Beta-3 adrenergic receptorHomo sapiens (human)Ki12.765011
Bile salt export pumpHomo sapiens (human)IC5015.800033
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Cytochrome P450 1A2Homo sapiens (human)IC500.019011
Cytochrome P450 2C9 Homo sapiens (human)IC500.300011
Cytochrome P450 2J2Homo sapiens (human)IC500.031834
Cytochrome P450 2J2Homo sapiens (human)Ki0.020012
D(1A) dopamine receptorHomo sapiens (human)IC5020.449011
D(1A) dopamine receptorHomo sapiens (human)Ki10.225011
D(3) dopamine receptorHomo sapiens (human)IC5028.860011
D(3) dopamine receptorHomo sapiens (human)Ki9.800011
Estrogen receptorHomo sapiens (human)IC504.545044
Estrogen receptorHomo sapiens (human)Ki1.272944
Estrogen receptor betaHomo sapiens (human)Ki0.002933
Glucocorticoid receptorHomo sapiens (human)IC504.314011
Glucocorticoid receptorHomo sapiens (human)Ki1.961011
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)IC504.314011
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki1.961011
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)IC504.314011
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki1.961011
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC504.314011
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki1.961011
Glycine receptor subunit betaRattus norvegicus (Norway rat)IC504.314011
Glycine receptor subunit betaRattus norvegicus (Norway rat)Ki1.961011
Gonadotropin-releasing hormone receptorHomo sapiens (human)IC500.000533
Gonadotropin-releasing hormone receptorRattus norvegicus (Norway rat)IC500.000633
Gonadotropin-releasing hormone receptorRattus norvegicus (Norway rat)Ki5,370,320,000,000,000.000011
Kappa-type opioid receptorHomo sapiens (human)IC5015.518011
Kappa-type opioid receptorHomo sapiens (human)Ki6.207011
Mu-type opioid receptorHomo sapiens (human)IC5014.079011
Mu-type opioid receptorHomo sapiens (human)Ki5.715011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC5017.747011
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki3.762011
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)Ki0.004611
Sodium-dependent dopamine transporter Homo sapiens (human)IC506.842011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki5.436011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC505.698011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki5.651011
Sodium-dependent serotonin transporterHomo sapiens (human)IC5015.420011
Sodium-dependent serotonin transporterHomo sapiens (human)Ki8.193011
Substance-K receptorHomo sapiens (human)IC5026.580011
Substance-K receptorHomo sapiens (human)Ki8.860011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Sex hormone-binding globulinHomo sapiens (human)Kd0.006311