Roles > estrogen receptor agonist
Page last updated: 2024-08-05 15:34:41

estrogen receptor agonist

An agonist at the estrogen receptor.

ChEBI ID: 63951

Members (9)

MemberDefinitionClass
1,3,5-tris(4-hydroxyphenyl)-4-propyl-1h-pyrazoleA pyrazole that is 1H-pyrazole bearing three 4-hydroxyphenyl substituents at positions 1, 3 and 5 as well as a propyl substituent at position 4. Potent, subtype-selective estrogen receptor agonist (EC50 ~ 200 pM); displays 410-fold selectivity for ERalpha over ERbeta. Prevents ovariectomy-induced weight gain and loss of bone mineral density, and induces gene expression in the hypothalamus following systemic administration in vivo.4,4',4''-(4-propylpyrazole-1,3,5-triyl)trisphenol
2,3-bis(4-hydroxyphenyl)-propionitrileA nitrile that is acetonitrile in which one of the hydrogens is replaced by a 4-hydroxyphenyl group while a second hydrogen is replaced by a 4-hydroxybenzyl group. It is a specific agonist for estrogen receptor beta (ERbeta).2,3-bis(4-hydroxyphenyl)propionitrile
5,11-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diolA 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
estetrolA 3-hydroxy steroid that is 17beta-estradiol which has been substituted at the 15alpha and 16alpha positions by two additional hydroxy groups. It is a natural estrogen produced exclusively during pregnancy by the fetal liver.estetrol
estradiol 3-benzoateA benzoate ester resulting from the formal condensation of benzoic acid with the phenolic hydroxy group of 17beta-estradiol.17beta-estradiol 3-benzoate
fludioxonilA member of the class of benzodioxoles that is 2,2-difluoro-1,3-benzodioxole substituted at position 4 by a 3-cyanopyrrol-4-yl group. A fungicide seed treatment for control of a range of diseases including Fusarium, Rhizoctonia and Alternaria.fludioxonil
lasofoxifeneA 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
psoralidinA member of the class of coumestans that is coumestan substituted by hydroxy groups at positions 3 and 9 and a prenyl group at position 2 respectively.psoralidin
resolvin d2A member of the class of resolvins that is (4Z,8E,10Z,12E,14E,19Z)-docosahexaenoic acid carrying three hydroxy substituents at positions 7, 16 and 17 (the 7S,16R,17S-stereoisomer).resolvin D2

Research

Studies (1,818)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990161 (8.86)18.7374
1990's117 (6.44)18.2507
2000's632 (34.76)29.6817
2010's736 (40.48)24.3611
2020's172 (9.46)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials118 (6.13%)5.53%
Reviews63 (3.27%)6.00%
Case Studies5 (0.26%)4.05%
Observational0 (0.00%)0.25%
Other1,740 (90.34%)84.16%

Protein Targets (174)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency29.903312
15-lipoxygenase, partialHomo sapiens (human)Potency10.000012
67.9K proteinVaccinia virusPotency11.220211
acid sphingomyelinaseHomo sapiens (human)Potency25.118911
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.183812
alpha-galactosidaseHomo sapiens (human)Potency32.815235
Alpha-synucleinHomo sapiens (human)Potency18.356411
Amyloid-beta precursor proteinHomo sapiens (human)Potency29.092911
AR proteinHomo sapiens (human)Potency9.86331113
aryl hydrocarbon receptorHomo sapiens (human)Potency21.072633
ATAD5 protein, partialHomo sapiens (human)Potency30.163833
Ataxin-2Homo sapiens (human)Potency27.829812
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency37.933011
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency10.691011
beta-2 adrenergic receptorHomo sapiens (human)Potency34.062022
Bloom syndrome protein isoform 1Homo sapiens (human)Potency18.867724
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency59.621812
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency12.197211
caspase-3Homo sapiens (human)Potency12.197211
Cellular tumor antigen p53Homo sapiens (human)Potency28.205735
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency21.295024
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency31.950314
Chain A, Beta-lactamaseEscherichia coli K-12Potency58.334412
Chain A, CruzipainTrypanosoma cruziPotency31.939424
Chain A, Ferritin light chainEquus caballus (horse)Potency31.622811
Chain A, HADH2 proteinHomo sapiens (human)Potency15.849825
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency50.118711
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.002811
Chain B, HADH2 proteinHomo sapiens (human)Potency15.849825
chromobox protein homolog 1Homo sapiens (human)Potency52.076423
cytochrome P450 2C19 precursorHomo sapiens (human)Potency11.294712
cytochrome P450 2C9 precursorHomo sapiens (human)Potency3.162312
cytochrome P450 2C9, partialHomo sapiens (human)Potency33.785811
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency30.736913
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency9.180424
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency27.306011
D(1A) dopamine receptorHomo sapiens (human)Potency6.237823
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency28.370812
DNA polymerase eta isoform 1Homo sapiens (human)Potency100.000011
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency28.183811
DNA polymerase kappa isoform 1Homo sapiens (human)Potency2.511911
dopamine D1 receptorHomo sapiens (human)Potency23.109311
endonuclease IVEscherichia coliPotency50.118711
estrogen nuclear receptor alphaHomo sapiens (human)Potency18.42701015
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency17.228911
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency20.14391013
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.543815
farnesoid X nuclear receptorHomo sapiens (human)Potency27.308424
GVesicular stomatitis virusPotency33.785811
GABA theta subunitRattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency9.180412
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency9.180412
gemininHomo sapiens (human)Potency20.923647
GLI family zinc finger 3Homo sapiens (human)Potency13.458722
glp-1 receptor, partialHomo sapiens (human)Potency15.237923
GLS proteinHomo sapiens (human)Potency12.356623
glucocerebrosidaseHomo sapiens (human)Potency25.110615
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency24.669336
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency24.336511
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency44.668411
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency4.1957210
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency44.716412
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency33.785811
huntingtin isoform 2Homo sapiens (human)Potency11.220211
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency43.641211
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency14.140624
IDH1Homo sapiens (human)Potency18.356411
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency33.785812
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency19.952611
Integrin alpha-IIbHomo sapiens (human)Potency23.735812
Integrin beta-3Homo sapiens (human)Potency23.735812
Interferon betaHomo sapiens (human)Potency33.785811
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency50.118712
lamin isoform A-delta10Homo sapiens (human)Potency10.042225
lethal factor (plasmid)Bacillus anthracis str. A2012Potency15.848912
LuciferasePhotinus pyralis (common eastern firefly)Potency16.944111
M-phase phosphoprotein 8Homo sapiens (human)Potency37.646012
Microtubule-associated protein tauHomo sapiens (human)Potency25.125423
mitogen-activated protein kinase 1Homo sapiens (human)Potency29.105623
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency13.457423
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency79.432811
neuropeptide S receptor isoform AHomo sapiens (human)Potency11.294712
NFKB1 protein, partialHomo sapiens (human)Potency19.091924
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency22.740612
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.047911
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency47.869324
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency20.596211
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency44.668411
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency48.966211
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency16.531122
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency27.426833
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency50.118711
ParkinHomo sapiens (human)Potency13.994322
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency3.612511
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency40.247212
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency31.425436
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency25.665122
plasminogen precursorMus musculus (house mouse)Potency7.943311
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency19.118012
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency5.745712
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency14.140612
pregnane X nuclear receptorHomo sapiens (human)Potency21.577422
pregnane X receptorRattus norvegicus (Norway rat)Potency64.775812
progesterone receptorHomo sapiens (human)Potency17.247522
putative alpha-glucosidaseOryza sativa Japonica Group (Japanese rice)Potency39.810711
RAR-related orphan receptor gammaMus musculus (house mouse)Potency18.658222
ras-related protein Rab-9AHomo sapiens (human)Potency58.047911
regulator of G-protein signaling 4Homo sapiens (human)Potency25.228812
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency24.984622
retinoid X nuclear receptor alphaHomo sapiens (human)Potency19.443247
serine-protein kinase ATM isoform aHomo sapiens (human)Potency17.782811
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency16.481611
Smad3Homo sapiens (human)Potency35.481311
survival motor neuron protein isoform dHomo sapiens (human)Potency35.481311
TAR DNA-binding protein 43Homo sapiens (human)Potency22.740612
TDP1 proteinHomo sapiens (human)Potency19.435825
thioredoxin reductaseRattus norvegicus (Norway rat)Potency39.071349
ThrombopoietinHomo sapiens (human)Potency6.477624
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency12.683722
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency24.803312
thyroid stimulating hormone receptorHomo sapiens (human)Potency16.413936
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency2.511911
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency27.621123
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency7.943311
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency7.943311
USP1 protein, partialHomo sapiens (human)Potency56.234111
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency19.284123
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency60.374012
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency24.336511
VprHuman immunodeficiency virus 1Potency35.481311

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC5011.565011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki7.359011
Adenosine receptor A3Homo sapiens (human)IC5021.780011
Adenosine receptor A3Homo sapiens (human)Ki12.312011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC5017.229011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki17.087011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC5021.780011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki12.312011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC5021.780011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki12.312011
Alpha-2C adrenergic receptorHomo sapiens (human)IC5024.650011
Alpha-2C adrenergic receptorHomo sapiens (human)Ki3.582011
Androgen receptorRattus norvegicus (Norway rat)IC500.010011
Androgen receptorRattus norvegicus (Norway rat)Ki0.007011
Bile acid receptorHomo sapiens (human)IC501.310011
Estrogen receptorHomo sapiens (human)IC500.0101911
Estrogen receptorRattus norvegicus (Norway rat)IC500.011212
Estrogen receptorHomo sapiens (human)Ki0.018011
Estrogen receptor betaHomo sapiens (human)IC500.0077810
Estrogen receptor betaRattus norvegicus (Norway rat)IC500.011212
Glucocorticoid receptorHomo sapiens (human)IC505.074011
Glucocorticoid receptorHomo sapiens (human)Ki2.306011
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)IC505.074011
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki2.306011
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)IC505.074011
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki2.306011
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC505.074011
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki2.306011
Glycine receptor subunit betaRattus norvegicus (Norway rat)IC505.074011
Glycine receptor subunit betaRattus norvegicus (Norway rat)Ki2.306011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusKi2.950012
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC5017.229011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki17.087011
Sodium-dependent serotonin transporterHomo sapiens (human)IC503.672011
Sodium-dependent serotonin transporterHomo sapiens (human)Ki1.951011
Tyrosine-protein kinase FynHomo sapiens (human)IC5022.994011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Arachidonate 5-lipoxygenase-activating proteinHomo sapiens (human)Kd21.000011
Cytochrome P450 2C9 Homo sapiens (human)EC502.300011
Estrogen receptorHomo sapiens (human)EC501.25011213
Estrogen receptorRattus norvegicus (Norway rat)EC502.431012
Estrogen receptor betaHomo sapiens (human)EC50115.71831414
Estrogen receptor betaRattus norvegicus (Norway rat)EC502.431012
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC508.600011
recombinase AMycobacterium tuberculosis H37RvEC50110.590022
Sex hormone-binding globulinHomo sapiens (human)Kd1.148211
streptokinase A precursorStreptococcus pyogenes M1 GASEC502.177522

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
heat shock protein 90, putativePlasmodium falciparum 3D7AC507.757011
heat shock protein HSP 90-alpha isoform 2Homo sapiens (human)AC506.320011
replicative DNA helicaseMycobacterium tuberculosis H37RvAC503.641022
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