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receptor antagonist activity

Definition

Target type: molecularfunction

The activity of a gene product that interacts with a receptor to decrease the ability of the receptor agonist to bind and activate the receptor. [GOC:ceb, ISBN:0198506732]

Receptor antagonist activity refers to the ability of a molecule to bind to a specific receptor and block the binding of its natural ligand. This binding event prevents the receptor from initiating its downstream signaling pathway, thereby inhibiting the biological response that would normally occur. Receptor antagonists are often used in medicine to treat a variety of conditions, including hypertension, asthma, and allergies. They can also be used to study the function of receptors in the body. The molecular mechanism of receptor antagonism involves the antagonist molecule binding to the receptor's active site, often with a high affinity, preventing the ligand from binding. This binding can be reversible or irreversible, depending on the specific antagonist and receptor. For reversible antagonists, the antagonist binds to the receptor and then dissociates, allowing the ligand to bind again. Irreversible antagonists permanently bind to the receptor, effectively inactivating it. In addition to blocking the binding of the natural ligand, receptor antagonists can also induce conformational changes in the receptor, further inhibiting its activity. These conformational changes can alter the receptor's ability to interact with other proteins involved in signaling pathways, further preventing the transmission of the signal. The selectivity of receptor antagonists is crucial for their therapeutic efficacy. A highly selective antagonist will only bind to its target receptor and not to other receptors, minimizing the risk of off-target effects. However, some receptor antagonists can exhibit non-selective binding, leading to unwanted side effects. The development of receptor antagonists is a complex process that involves understanding the structure and function of the target receptor, identifying potential antagonists, and evaluating their efficacy and safety. This knowledge is crucial for the design of new and effective therapeutic agents for a wide range of diseases.'
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Proteins (4)

ProteinDefinitionTaxonomy
Estrogen receptor betaAn estrogen receptor beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92731]Homo sapiens (human)
Type-2 angiotensin II receptorAn angiotensin II receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P50052]Homo sapiens (human)
All-trans-retinol dehydrogenase [NADAn all-trans-retinol dehydrogenase [NAD(+)] ADH7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P40394]Homo sapiens (human)
Dickkopf-related protein 1A dickkopf-related protein 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O94907]Homo sapiens (human)

Compounds (127)

CompoundDefinitionClassesRoles
naringenin4'-hydroxyflavanones;
trihydroxyflavanone
tetramethylene sulfoxidetetrahydrothiophenes
5-iodo-2-(oxaloamino)benzoic acidorganoiodine compound
candesartancandesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.

candesartan: a nonpeptide angiotensin II receptor antagonist
benzimidazolecarboxylic acid;
biphenylyltetrazole
angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
stallimycin
emodinemodin : A trihydroxyanthraquinone that is 9,10-anthraquinone which is substituted by hydroxy groups at positions 1, 3, and 8 and by a methyl group at position 6. It is present in the roots and barks of numerous plants (particularly rhubarb and buckthorn), moulds, and lichens. It is an active ingredient of various Chinese herbs.

Emodin: Purgative anthraquinone found in several plants, especially RHAMNUS PURSHIANA. It was formerly used as a laxative, but is now used mainly as a tool in toxicity studies.
trihydroxyanthraquinoneantineoplastic agent;
laxative;
plant metabolite;
tyrosine kinase inhibitor
avaproirbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.

Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.
azaspiro compound;
biphenylyltetrazole
angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
losartanlosartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position

Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
biphenylyltetrazole;
imidazoles
angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
miconazole1-[2-(2,4-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 2,4-dichlorobenzyl group.

miconazole : A racemate composed of equimolar amounts of (R)- and (S)-miconazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes.

Miconazole: An imidazole antifungal agent that is used topically and by intravenous infusion.
dichlorobenzene;
ether;
imidazoles
raloxifeneraloxifene : 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.1-benzothiophenes;
aromatic ketone;
N-oxyethylpiperidine;
phenols
bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
prednisoloneprednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.

Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.
11beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone
adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
drug metabolite;
environmental contaminant;
immunosuppressive agent;
xenobiotic
spironolactonespironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7.

Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827)
3-oxo-Delta(4) steroid;
oxaspiro compound;
steroid lactone;
thioester
aldosterone antagonist;
antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
estroneHydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens.17-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols
antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite
ethinyl estradiol17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.

Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.
17-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound
xenoestrogen
medroxyprogesterone acetate20-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
corticosteroid;
steroid ester
adjuvant;
androgen;
antineoplastic agent;
antioxidant;
female contraceptive drug;
inhibitor;
progestin;
synthetic oral contraceptive
bisphenol a4,4'-isopropylidene diphenol: stimulates proliferative responses and cytokine productions of murine spleen cells and thymus cells in vitro

bisphenol : By usage, the methylenediphenols, HOC6H4CH2C6H4OH, commonly p,p-methylenediphenol, and their substitution products (generally derived from condensation of two equivalent amounts of a phenol with an aldehyde or ketone). The term also includes analogues in the the methylene (or substituted methylene) group has been replaced by a heteroatom.

bisphenol A : A bisphenol that is 4,4'-methanediyldiphenol in which the methylene hydrogens are replaced by two methyl groups.
bisphenolendocrine disruptor;
environmental contaminant;
xenobiotic;
xenoestrogen
2,6-dihydroxyanthraquinone2,6-dihydroxyanthraquinone: structure given in first source

anthraflavic acid : A dihydroxyanthraquinone that is anthracene substituted by hydroxy groups at C-3 and C-7 and oxo groups at C-9 and C-10.
dihydroxyanthraquinoneantimutagen;
plant metabolite
ethyl-p-hydroxybenzoateethyl-p-hydroxybenzoate: structureethyl ester;
paraben
antifungal agent;
antimicrobial food preservative;
phytoestrogen;
plant metabolite
androstenediolandrost-5-ene-3beta,17beta-diol : A 3beta-hydroxy-Delta(5)-steroid that is 3beta-hydroxyandrost-5-ene carrying an additional hydroxy group at position 17beta.

Androstenediol: An intermediate in TESTOSTERONE biosynthesis, found in the TESTIS or the ADRENAL GLANDS. Androstenediol, derived from DEHYDROEPIANDROSTERONE by the reduction of the 17-keto group (17-HYDROXYSTEROID DEHYDROGENASES), is converted to TESTOSTERONE by the oxidation of the 3-beta hydroxyl group to a 3-keto group (3-HYDROXYSTEROID DEHYDROGENASES).
17beta-hydroxy steroid;
3beta-hydroxy-Delta(5)-steroid
androgen;
human metabolite;
mouse metabolite;
radiation protective agent
isovaleramideisovaleramide: inhibits liver alcohol dehydrogenases
4-cumylphenoldiarylmethane
4,4'-bisphenol f4,4'-bisphenol F: RN given refers to parent cpd

bisphenol F : A bisphenol that is methane in which two of the hydrogens have been replaced by 4-hydroxyphenyl groups.
bisphenol;
diarylmethane
environmental food contaminant;
xenoestrogen
n-cyclohexylformamidealicyclic compound;
formamides
mouse metabolite
levormeloxifenelevormeloxifene: RN refers to (trans)-isomer
raloxifene hydrochlorideraloxifene hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride.

Raloxifene Hydrochloride: A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.
hydrochloridebone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
mifepristoneMifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.3-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound
abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive
ipsapironeN-arylpiperazine
flesinoxan
valsartanvalsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.

Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.
biphenylyltetrazole;
monocarboxylic acid;
monocarboxylic acid amide
angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
1,1-bis(4-hydroxyphenyl)-2-phenylbut-1-ene1,1-bis(4-hydroxyphenyl)-2-phenylbut-1-ene: structure given in first source
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenolstilbenoid
taleranoltaleranol: a metabolite of ZEARALENONE which is a non-steroidal estrogenic lactone used as an anabolic compound in animal feed; a stereoisomer of ZERANOL (alpha-zearalanol)macrolide
telmisartantelmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.

Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.
benzimidazoles;
biphenyls;
carboxybiphenyl
angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
6-ketoestradiol
alfatradiol17alpha-estradiol : An estradiol that is estra-1,3,5(10)-triene substituted by hydroxy groups at positions 3 and 17 (the 17alpha stereoisomer).

alfatradiol: used for treating androgenetic alopecia
17alpha-hydroxy steroid;
3-hydroxy steroid;
estradiol
estrogen;
geroprotector
2,2-bis(4-hydroxyphenyl)-1,1,1-trichloroethane2,2-bis(4-hydroxyphenyl)-1,1,1-trichloroethane: methoxychlor metabolitebisphenol
n-benzylformamideformamides
bexarotenebenzoic acids;
naphthalenes;
retinoid
antineoplastic agent
equolEquol: A non-steroidal ESTROGEN generated when soybean products are metabolized by certain bacteria in the intestines.hydroxyisoflavans
anthraglycoside banthraglycoside B: from Polygonum cuspidatum Sieb. et Zucc; structure in first sourcedihydroxyanthraquinone
effusoleffusol: from the pith of Juncus effusus L.; structure in first source
2,3-bis(4-hydroxyphenyl)-propionitrile2,3-bis(4-hydroxyphenyl)-propionitrile: a selective estrogen receptor beta agonist or modulator. also called DPN compound

2,3-bis(4-hydroxyphenyl)propionitrile : A 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).
nitrile;
phenols
estrogen receptor agonist
fulvestrantfulvestrant : 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: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.
17beta-hydroxy steroid;
3-hydroxy steroid;
organofluorine compound;
sulfoxide
antineoplastic agent;
estrogen antagonist;
estrogen receptor antagonist
ici 164384ICI 164384: structure given in first source

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.
17beta-hydroxy steroid;
3-hydroxy steroid;
tertiary carboxamide
anti-estrogen;
antineoplastic agent;
estrogen receptor antagonist
ly 117018LY 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: from Eli Lilly; less estrogenic & more estrogen-antagonistic than tamoxifen & trioxifene in rats & mice; LY 139478 is the HCl salt of LY 117018; LY 139478 is an estrogen agonist; structure in first source; a raloxifene analog
1-benzothiophenes;
aromatic ketone;
N-alkylpyrrolidine;
phenols
bone density conservation agent;
estrogen receptor antagonist;
estrogen receptor modulator
Zearalanonemacrolide;
resorcinols
liquiritigenin4',7-dihydroxyflavanone : A dihydroxyflavanone in which the two hydroxy substituents are located at positions 4' and 7.

liquiritigenin : A dihydroxyflavanone compound having the two hydroxy substituents at the 4'- and 7-positions. Isolated from the root of Glycyrrhizae uralensis, it is a selective agonist for oestrogen receptor beta.

liquiritigenin: structure given in first source; isolated from Pterocarpus marsupium
4',7-dihydroxyflavanonehormone agonist;
plant metabolite
estrone-3-o-sulfamateestrone-3-O-sulfamate: a steroid sulfatase inhibitor
exp7711EXP7711: to search, use E#P7711(nm); angiotensin II receptor antagonist; structure given in first source
zk 119010ZK 119010: possess both antagonistic and agonistic potencies in MCF-7 cells
bibs 39BIBS 39: structure given in first source; angiotensin II receptor antagonist
a 81988A 81988: angiotensin II antagonist selective for type 1 receptors
bibs 222BIBS 222: structure given in first source; angiotensin II receptor antagonist
bazedoxifenephenylindole
chrysamine gchrysamine G: structure given in first source; RN refers to disodium salt
angiotensin iiGiapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock

Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).
amino acid zwitterion;
angiotensin II
human metabolite
ly 353381LY 353381: structure in first source
l 158809L 158809: RN & structure given in first source; angiotensin receptor antagonist
lasofoxifenelasofoxifene : A 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: structure in first source
aromatic ether;
N-alkylpyrrolidine;
naphthols;
tetralins
antineoplastic agent;
bone density conservation agent;
cardioprotective agent;
estrogen receptor agonist;
estrogen receptor antagonist
1,1-bis(4-hydroxyphenyl)cyclohexane1,1-bis(4-hydroxyphenyl)cyclohexane: structure in first sourcediarylmethane
2-hydroxyestradiol2-hydroxy-17beta-estradiol : A 2-hydroxy steroid that consists of 17beta-estradiol having an additional hydroxy group at position 2.

2-hydroxyestradiol: catechol estrogen; RN given refers to (17 beta)-isomer
17beta-hydroxy steroid;
2-hydroxy steroid
carcinogenic agent;
human metabolite;
metabolite;
mouse metabolite;
prodrug
naringenin(S)-naringenin : The (S)-enantiomer of naringenin.(2S)-flavan-4-one;
naringenin
expectorant;
plant metabolite
davidigenindavidigenin : A member of the class of dihydrochalcones that is dihydrochalcone substituted by hydroxy groups at positions 4, 2', and 4' respectively.

davidigenin: has antispasmodic activity; isolated from Mascarenhasia arborescens; structure in first source
dihydrochalcones;
polyphenol
anti-allergic agent;
anti-asthmatic agent;
antioxidant;
metabolite
eplerenoneEplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION.3-oxo-Delta(4) steroid;
epoxy steroid;
gamma-lactone;
methyl ester;
organic heteropentacyclic compound;
oxaspiro compound;
steroid acid ester
aldosterone antagonist;
antihypertensive agent
fluticasone propionatefluticasone propionate : A trifluorinated corticosteroid that consists of 6alpha,9-difluoro-11beta,17alpha-dihydroxy-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-16-methyl-3-oxoandrosta-1,4-diene bearing a propionyl substituent at position 17; has anti-inflammatory, anti-asthmatic and anti-allergic activity.11beta-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
corticosteroid;
fluorinated steroid;
propanoate ester;
steroid ester;
thioester
adrenergic agent;
anti-allergic agent;
anti-asthmatic drug;
anti-inflammatory drug;
bronchodilator agent;
dermatologic drug
2-(oxaloamino)benzoic acid(oxaloamino)benzoic acid
diethylstilbestroldiethylstilbestrol : An olefinic compound that is trans-hex-3-ene in which the hydrogens at positions 3 and 4 have been replaced by p-hydroxyphenyl groups.

Diethylstilbestrol: A synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders. It was also used formerly as a growth promoter in animals. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), diethylstilbestrol has been listed as a known carcinogen. (Merck, 11th ed)
olefinic compound;
polyphenol
antifungal agent;
antineoplastic agent;
autophagy inducer;
calcium channel blocker;
carcinogenic agent;
EC 1.1.1.146 (11beta-hydroxysteroid dehydrogenase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
endocrine disruptor;
xenoestrogen
alitretinoinAlitretinoin: A retinoid that is used for the treatment of chronic hand ECZEMA unresponsive to topical CORTICOSTEROIDS. It is also used to treat cutaneous lesions associated with AIDS-related KAPOSI SARCOMA.retinoic acidantineoplastic agent;
keratolytic drug;
metabolite;
retinoid X receptor agonist
afimoxifeneafimoxifene : A tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen.phenols;
tertiary amino compound
antineoplastic agent;
estrogen receptor antagonist;
metabolite
8-prenylnaringenin8-prenylnaringenin: a phytogenic antineoplastic agent; structure in first source

sophoraflavanone B : A trihydroxyflavanone that is (S)-naringenin having a prenyl group at position 8.
(2S)-flavan-4-one;
4'-hydroxyflavanones;
trihydroxyflavanone
plant metabolite;
platelet aggregation inhibitor
8-isopentenylnaringenin8-isopentenylnaringenin: a non-steroidal phytoestrogen from Anaxagorea luzonensis; structure in first sourceflavanones
1,1-Bis(4-hydroxyphenyl)ethanediarylmethane
trans-4-coumaric acid4-coumaric acid : A coumaric acid in which the hydroxy substituent is located at C-4 of the phenyl ring.

hydroxycinnamic acid : Any member of the class of cinnamic acids carrying one or more hydroxy substituents.

trans-4-coumaric acid : The trans-isomer of 4-coumaric acid.
4-coumaric acidfood component;
mouse metabolite;
plant metabolite
isoliquiritigeninchalconesantineoplastic agent;
biological pigment;
EC 1.14.18.1 (tyrosinase) inhibitor;
GABA modulator;
geroprotector;
metabolite;
NMDA receptor antagonist
2,4,4'-trihydroxydeoxybenzoin2,4,4'-trihydroxydeoxybenzoin: structure in first source
erb 041ERB 041: an estrogen receptor beta agonist; structure in first source
tamoxifen citratecitrate saltangiogenesis inhibitor;
anticoronaviral agent
tamoxifenstilbenoid;
tertiary amino compound
angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
zeranolZeranol: A non-steroidal estrogen analog.macrolide
idoxifeneidoxifene: structure given in first sourcestilbenoid
tak 013
N-[2-(2-methyl-1-indolyl)ethyl]benzamideindoles
apigeninChamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia.trihydroxyflavoneantineoplastic agent;
metabolite
genistein7-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
pulmicortbudesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis.

Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.
11beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic acetal;
glucocorticoid;
primary alpha-hydroxy ketone
anti-inflammatory drug;
bronchodilator agent;
drug allergen
zearalenonezearalenone : A macrolide comprising a fourteen-membered lactone fused to 1,3-dihydroxybenzene; a potent estrogenic metabolite produced by some Giberella species.

Zearalenone: (S-(E))-3,4,5,6,8,10-Hexahydro-14,16-dihydroxy-3-methyl-1H-2-benzoxacyclotetradecin-1,7(8H)-dione. One of a group of compounds known under the general designation of resorcylic acid lactones. Cis, trans, dextro and levo forms have been isolated from the fungus Gibberella zeae (formerly Fusarium graminearum). They have estrogenic activity, cause toxicity in livestock as feed contaminant, and have been used as anabolic or estrogen substitutes.
macrolide;
resorcinols
fungal metabolite;
mycoestrogen
coumestrolcoumestrol : A member of the class of coumestans that is coumestan with hydroxy substituents at positions 3 and 9.

Coumestrol: A daidzein derivative occurring naturally in forage crops which has some estrogenic activity.
coumestans;
delta-lactone;
polyphenol
anti-inflammatory agent;
antioxidant;
plant metabolite
daidzein7-hydroxyisoflavonesantineoplastic agent;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
phytoestrogen;
plant metabolite
4-hydroxyestradiol4-hydroxy-17beta-estradiol : A 4-hydroxy steroid that consists of 17beta-estradiol having an additional hydroxy group at position 4.

4-hydroxyestradiol: catechol estrogen
4-hydroxy steroidmetabolite
afimoxifene
gw 56383-(4-(1,2-diphenylbut-1-enyl)phenyl)acrylic acid: exhibits estrogen agonist activity in bone and estrogen antagonist activity in uterus; structure in first source
pd 123319PD123319 : An imidazopyridine consisting of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine having 4-(dimethylamino)-3-methylbenzyl, diphenylacetyl and carboxy and groups at positions 1, 5 and 6 respectivelyimidazopyridineangiotensin receptor antagonist;
endothelin receptor antagonist;
vasoconstrictor agent
exp 655
onapristoneonapristone: induces vaginal bleeding and luteal regression in monkeys; structure given in first source; progesterone antagonist
broussonin abroussonin A: has antiviral activity; isolated from Anemarrhena asphodeloides; structure in first source
1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)ethanone1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta(c)quinolin-8-yl)ethanone: G-1 was able to induce both c-fos expression and proliferation in the ERalpha-negative/GPR30-positive SKBR3 breast cancer cells, the requirement for ERalpha expression in GPR30/EGFR signaling may depend on the specific cellular context of different tumor typesagonist
4-[(3aR,4S,9bS)-8-[(4-methoxyphenyl)sulfamoyl]-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-4-yl]benzoic acidquinolines
ly2066948LY2066948: a selective estrogen receptor modulator; structure in first source
afimoxifene
dehydrodiconiferyl alcoholdehydrodiconiferyl alcohol : A guaiacyl lignin obtained by cyclodimerisation of coniferol.

dehydrodiconiferyl alcohol: structure given in first source
1-benzofurans;
guaiacols;
guaiacyl lignin;
primary alcohol
anti-inflammatory agent;
plant metabolite
way 2021963-(3-fluoro-4-hydroxyphenyl)-7-hydroxy-1-naphthonitrile: structure in first source
saralasinSaralasin: An octapeptide analog of angiotensin II (bovine) with amino acids 1 and 8 replaced with sarcosine and alanine, respectively. It is a highly specific competitive inhibitor of angiotensin II that is used in the diagnosis of HYPERTENSION.oligopeptide
era-9232-(4-hydroxyphenyl)-3-methyl-1-(4-(2-piperidin-1-yl-ethoxy)-benzyl)-1H-indol-5-ol: structure in first source
pregna-4,17-diene-3,16-dionepregna-4,17-diene-3,16-dione: steroid from guggulu extract; RN & N1 from C1 Form index; RN given refers to cpd without isomeric designation; structure in first source; antagonist of farnesoid X receptor3-hydroxy steroidandrogen
pregna-4,17-diene-3,16-dione, (17z)-isomer
l 162313L 162313: a biphenylimidazole derivative; a non-peptide angiotensin agonist; no further information available 2/95
2-methyl-5-[(2-oxo-1H-benzo[cd]indol-6-yl)sulfonylamino]-3-benzofurancarboxylic acid butyl esternaphthalenes;
sulfonic acid derivative
gw 7604GW 7604: structure in first source
l 163491L 163491: structure given in first source
fluticasone furoatefluticasone furoate : A trifluorinated corticosteroid that consists of 6alpha,9-difluoro-11beta,17alpha-dihydroxy-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-16-methyl-3-oxoandrosta-1,4-diene bearing a 2-furoyl substituent at position 17. Used in combination with vilanterol trifenate for treatment of bronchospasm associated with chronic obstructive pulmonary disease.

fluticasone furoate: a glucocorticoid; structure in first source
11beta-hydroxy steroid;
2-furoate ester;
3-oxo-Delta(1),Delta(4)-steroid;
corticosteroid;
fluorinated steroid;
steroid ester;
thioester
anti-allergic agent;
anti-asthmatic drug;
prodrug
nrx 194204IRX4204: retinoid X receptor (RXR) agonist; structure in first source
agn 194204AGN 194204: a retinoid X receptor ligand; structure in first source
em 800EM 800: EM-800 is the prodrug of EM-652; EM-800 and EM-776 are (S)- and (R)-isomers, respectively; structure in first source
ema401
6-(3-hydroxyphenyl)-2-naphthol6-(3-hydroxyphenyl)-2-naphthol: has inhibitory effects on tyrosinase activity and melanin synthesis; structure in first source
licoflavone clicoflavone C: Antimutagenic Agent; a naturally occurring prenyl-flavone extracted from Genista ephedroides; structure in first source
erteberelerteberel: an estrogen receptor beta agonist
ly3201LY3201: estrogen receptor beta agonist
4-(2-phenyl-5,7-bis(trifluoromethyl)pyrazolo(1,5-a)pyrimidin-3-yl)phenol4-(2-phenyl-5,7-bis(trifluoromethyl)pyrazolo(1,5-a)pyrimidin-3-yl)phenol: a selective estrogen receptor modulatorpyrazoles;
ring assembly
ascochlorinascochlorin : A dihydroxybenzaldehyde that is 2,4-dihydroxybenzaldehyde which is substituted by a (1E,3E)-3-methyl-1-[(1R,2R,6R)-1,2,6-trimethyl-3-oxocyclohexyl]penta-1,3-dien-5-yl group at position 3, chlorine at position 5, and a methyl group at position 6. A meroterpenoid produced by several fungi including Ascochyta viciae . It exhibits anticancer, antifungal and antiprotozoal activities.

ascochlorin: structure in first source
cyclohexanones;
dihydroxybenzaldehyde;
meroterpenoid;
monochlorobenzenes;
olefinic compound;
resorcinols;
sesquiterpenoid
angiogenesis inhibitor;
antifungal agent;
antineoplastic agent;
antiprotozoal drug;
fungal metabolite
naluzotannaluzotan: an antidepressant and anti-anxiety agent; structure in first source
y134 compoundY134 compound: a selective estrogen receptor modulator derived from raloxifene; structure in first sourcearomatic ketone
moxestrolmoxestrol: RN given refers to (11beta,17alpha)-isomer; structure3-hydroxy steroid
(1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamineWAY-262611: a wingless beta-catenin agonist; structure in first sourcenaphthalenes
nitd 609NITD 609: an antimalarial and coccidiostat; structure in first source
way 200070WAY 200070: a neuroprotective agent; structure in first source
way-169916WAY-169916: nonsteroidal selective NF-kappaB inhibitor; structure in first source