Page last updated: 2024-08-07 17:21:03
Estrogen receptor beta
An estrogen receptor beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92731]
Synonyms
ER-beta;
Nuclear receptor subfamily 3 group A member 2
Research
Bioassay Publications (142)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 13 (9.15) | 18.2507 |
2000's | 83 (58.45) | 29.6817 |
2010's | 35 (24.65) | 24.3611 |
2020's | 11 (7.75) | 2.80 |
Compounds (93)
Drugs with Potency Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
mifepristone | Homo sapiens (human) | Potency | 1.0000 | 1 | 1 |
onapristone | Homo sapiens (human) | Potency | 1.0000 | 1 | 1 |
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
naringenin | Homo sapiens (human) | IC50 | 42.8875 | 1 | 2 |
stallimycin | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
emodin | Homo sapiens (human) | IC50 | 5.2000 | 1 | 1 |
emodin | Homo sapiens (human) | Ki | 1.5000 | 1 | 1 |
raloxifene | Homo sapiens (human) | IC50 | 0.3051 | 40 | 43 |
raloxifene | Homo sapiens (human) | Ki | 0.0065 | 7 | 8 |
prednisolone | Homo sapiens (human) | IC50 | 55.0000 | 2 | 2 |
prednisolone | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
spironolactone | Homo sapiens (human) | IC50 | 46.6667 | 3 | 3 |
estrone | Homo sapiens (human) | IC50 | 0.3743 | 5 | 6 |
ethinyl estradiol | Homo sapiens (human) | IC50 | 0.0129 | 2 | 2 |
medroxyprogesterone acetate | Homo sapiens (human) | IC50 | 0.9240 | 2 | 2 |
bisphenol a | Homo sapiens (human) | IC50 | 0.8700 | 1 | 1 |
2,6-dihydroxyanthraquinone | Homo sapiens (human) | IC50 | 2.4000 | 1 | 1 |
2,6-dihydroxyanthraquinone | Homo sapiens (human) | Ki | 0.6900 | 1 | 1 |
androstenediol | Homo sapiens (human) | IC50 | 0.0100 | 2 | 2 |
4-cumylphenol | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
levormeloxifene | Homo sapiens (human) | IC50 | 0.0730 | 1 | 1 |
raloxifene hydrochloride | Homo sapiens (human) | IC50 | 0.1297 | 5 | 5 |
mifepristone | Homo sapiens (human) | IC50 | 3.5140 | 4 | 4 |
mifepristone | Homo sapiens (human) | Ki | 4.5420 | 3 | 3 |
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol | Homo sapiens (human) | IC50 | 0.0527 | 14 | 14 |
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol | Homo sapiens (human) | Ki | 0.0009 | 7 | 7 |
alfatradiol | Homo sapiens (human) | IC50 | 0.9000 | 2 | 2 |
2,2-bis(4-hydroxyphenyl)-1,1,1-trichloroethane | Homo sapiens (human) | IC50 | 0.0504 | 2 | 2 |
equol | Homo sapiens (human) | IC50 | 5.5710 | 1 | 1 |
anthraglycoside b | Homo sapiens (human) | IC50 | 62.0000 | 1 | 1 |
anthraglycoside b | Homo sapiens (human) | Ki | 18.0000 | 1 | 1 |
effusol | Homo sapiens (human) | IC50 | 0.0120 | 1 | 1 |
fulvestrant | Homo sapiens (human) | IC50 | 0.0104 | 11 | 11 |
fulvestrant | Homo sapiens (human) | Ki | 0.0032 | 3 | 3 |
ici 164384 | Homo sapiens (human) | Ki | 0.0029 | 3 | 3 |
ly 117018 | Homo sapiens (human) | IC50 | 0.1200 | 1 | 1 |
zk 119010 | Homo sapiens (human) | IC50 | 0.2420 | 1 | 1 |
bazedoxifene | Homo sapiens (human) | IC50 | 0.0444 | 2 | 2 |
ly 353381 | Homo sapiens (human) | IC50 | 0.0985 | 3 | 4 |
lasofoxifene | Homo sapiens (human) | IC50 | 0.0077 | 8 | 10 |
1,1-bis(4-hydroxyphenyl)cyclohexane | Homo sapiens (human) | IC50 | 0.5600 | 1 | 1 |
naringenin | Homo sapiens (human) | IC50 | 13.4730 | 1 | 1 |
davidigenin | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
eplerenone | Homo sapiens (human) | IC50 | 60.0000 | 2 | 2 |
fluticasone propionate | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
diethylstilbestrol | Homo sapiens (human) | IC50 | 0.1588 | 4 | 4 |
diethylstilbestrol | Homo sapiens (human) | Ki | 0.0003 | 3 | 3 |
afimoxifene | Homo sapiens (human) | IC50 | 0.0102 | 3 | 4 |
8-prenylnaringenin | Homo sapiens (human) | IC50 | 0.0625 | 1 | 2 |
8-isopentenylnaringenin | Homo sapiens (human) | IC50 | 0.0680 | 1 | 1 |
1,1-Bis(4-hydroxyphenyl)ethane | Homo sapiens (human) | IC50 | 2.4000 | 1 | 1 |
isoliquiritigenin | Homo sapiens (human) | IC50 | 0.2690 | 1 | 1 |
erb 041 | Homo sapiens (human) | IC50 | 0.0050 | 2 | 2 |
tamoxifen citrate | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
tamoxifen | Homo sapiens (human) | IC50 | 1.2790 | 22 | 22 |
tamoxifen | Homo sapiens (human) | Ki | 0.0510 | 4 | 4 |
idoxifene | Homo sapiens (human) | IC50 | 0.0075 | 1 | 1 |
N-[2-(2-methyl-1-indolyl)ethyl]benzamide | Homo sapiens (human) | IC50 | 32.7000 | 1 | 0 |
apigenin | Homo sapiens (human) | IC50 | 7.0650 | 2 | 2 |
genistein | Homo sapiens (human) | IC50 | 2.0569 | 24 | 26 |
genistein | Homo sapiens (human) | Ki | 0.0123 | 2 | 1 |
pulmicort | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
coumestrol | Homo sapiens (human) | IC50 | 0.0131 | 2 | 3 |
daidzein | Homo sapiens (human) | IC50 | 1.6568 | 5 | 6 |
daidzein | Homo sapiens (human) | Ki | 0.3000 | 1 | 1 |
afimoxifene | Homo sapiens (human) | IC50 | 0.0036 | 1 | 1 |
gw 5638 | Homo sapiens (human) | IC50 | 0.0560 | 1 | 1 |
onapristone | Homo sapiens (human) | IC50 | 1.0000 | 2 | 2 |
onapristone | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
broussonin a | Homo sapiens (human) | IC50 | 1.8000 | 1 | 1 |
ly2066948 | Homo sapiens (human) | Ki | 0.0011 | 2 | 3 |
afimoxifene | Homo sapiens (human) | IC50 | 0.0013 | 2 | 2 |
dehydrodiconiferyl alcohol | Homo sapiens (human) | IC50 | 0.2865 | 1 | 1 |
way 202196 | Homo sapiens (human) | IC50 | 0.0027 | 1 | 1 |
era-923 | Homo sapiens (human) | IC50 | 0.0400 | 1 | 1 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
pregna-4,17-diene-3,16-dione, (17z)-isomer | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
pregna-4,17-diene-3,16-dione, (17z)-isomer | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
gw 7604 | Homo sapiens (human) | IC50 | 0.0405 | 4 | 4 |
gw 7604 | Homo sapiens (human) | Ki | 0.0100 | 1 | 1 |
fluticasone furoate | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
em 800 | Homo sapiens (human) | IC50 | 0.0007 | 2 | 2 |
em 800 | Homo sapiens (human) | Ki | 0.0040 | 4 | 4 |
6-(3-hydroxyphenyl)-2-naphthol | Homo sapiens (human) | IC50 | 0.0300 | 1 | 1 |
erteberel | Homo sapiens (human) | Ki | 0.0012 | 9 | 14 |
ly3201 | Homo sapiens (human) | Ki | 0.0031 | 4 | 6 |
4-(2-phenyl-5,7-bis(trifluoromethyl)pyrazolo(1,5-a)pyrimidin-3-yl)phenol | Homo sapiens (human) | Ki | 0.8333 | 2 | 3 |
y134 compound | Homo sapiens (human) | IC50 | 0.0339 | 2 | 2 |
moxestrol | Homo sapiens (human) | IC50 | 0.0027 | 2 | 2 |
nitd 609 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
way 200070 | Homo sapiens (human) | IC50 | 0.0018 | 2 | 3 |
way-169916 | Homo sapiens (human) | IC50 | 0.1060 | 1 | 1 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
raloxifene | Homo sapiens (human) | EC50 | 0.2600 | 1 | 1 |
spironolactone | Homo sapiens (human) | EC50 | 3.3000 | 1 | 1 |
estrone | Homo sapiens (human) | EC50 | 0.1632 | 9 | 9 |
ethinyl estradiol | Homo sapiens (human) | EC50 | 0.0035 | 3 | 3 |
medroxyprogesterone acetate | Homo sapiens (human) | EC50 | 0.9240 | 1 | 1 |
bisphenol a | Homo sapiens (human) | EC50 | 0.9285 | 2 | 2 |
ethyl-p-hydroxybenzoate | Homo sapiens (human) | EC50 | 1.8600 | 1 | 1 |
androstenediol | Homo sapiens (human) | EC50 | 0.0058 | 2 | 2 |
4,4'-bisphenol f | Homo sapiens (human) | EC50 | 1.9000 | 1 | 1 |
mifepristone | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
1,1-bis(4-hydroxyphenyl)-2-phenylbut-1-ene | Homo sapiens (human) | EC50 | 0.3069 | 3 | 3 |
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol | Homo sapiens (human) | EC50 | 0.0008 | 1 | 1 |
taleranol | Homo sapiens (human) | EC50 | 0.1460 | 1 | 2 |
6-ketoestradiol | Homo sapiens (human) | EC50 | 0.0382 | 1 | 0 |
alfatradiol | Homo sapiens (human) | EC50 | 0.6172 | 2 | 2 |
2,2-bis(4-hydroxyphenyl)-1,1,1-trichloroethane | Homo sapiens (human) | Kd | 0.0112 | 1 | 1 |
2,3-bis(4-hydroxyphenyl)-propionitrile | Homo sapiens (human) | EC50 | 115.7183 | 14 | 14 |
Zearalanone | Homo sapiens (human) | EC50 | 0.3490 | 1 | 2 |
liquiritigenin | Homo sapiens (human) | EC50 | 0.0365 | 1 | 1 |
estrone-3-o-sulfamate | Homo sapiens (human) | EC50 | 3.7000 | 1 | 1 |
2-hydroxyestradiol | Homo sapiens (human) | EC50 | 1.0820 | 2 | 2 |
eplerenone | Homo sapiens (human) | EC50 | 20.0000 | 1 | 1 |
diethylstilbestrol | Homo sapiens (human) | EC50 | 0.0045 | 2 | 2 |
8-prenylnaringenin | Homo sapiens (human) | EC50 | 0.0050 | 1 | 1 |
1,1-Bis(4-hydroxyphenyl)ethane | Homo sapiens (human) | EC50 | 1.3950 | 1 | 1 |
trans-4-coumaric acid | Homo sapiens (human) | EC50 | 4.8900 | 1 | 1 |
2,4,4'-trihydroxydeoxybenzoin | Homo sapiens (human) | EC50 | 0.5000 | 1 | 1 |
tamoxifen | Homo sapiens (human) | EC50 | 0.9808 | 3 | 5 |
zeranol | Homo sapiens (human) | EC50 | 0.0240 | 1 | 1 |
genistein | Homo sapiens (human) | EC50 | 0.1635 | 9 | 9 |
zearalenone | Homo sapiens (human) | EC50 | 0.1100 | 1 | 1 |
4-hydroxyestradiol | Homo sapiens (human) | EC50 | 0.2857 | 2 | 2 |
broussonin a | Homo sapiens (human) | EC50 | 0.5300 | 1 | 1 |
1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)ethanone | Homo sapiens (human) | EC50 | 0.1838 | 1 | 0 |
4-[(3aR,4S,9bS)-8-[(4-methoxyphenyl)sulfamoyl]-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-4-yl]benzoic acid | Homo sapiens (human) | EC50 | 2.2770 | 1 | 0 |
2-methyl-5-[(2-oxo-1H-benzo[cd]indol-6-yl)sulfonylamino]-3-benzofurancarboxylic acid butyl ester | Homo sapiens (human) | EC50 | 0.0837 | 1 | 0 |
licoflavone c | Homo sapiens (human) | EC50 | 0.0035 | 1 | 1 |
erteberel | Homo sapiens (human) | EC50 | 0.0007 | 1 | 1 |
Drugs with Other Measurements
Rational design, synthesis, antiproliferative activity against MCF-7, MDA-MB-231 cells, estrogen receptors binding affinity, and computational study of indenopyrimidine-2,5-dione analogs for the treatment of breast cancer.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 64, 2022
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Structural features underlying raloxifene's biophysical interaction with bone matrix.Bioorganic & medicinal chemistry, , 02-15, Volume: 24, Issue:4, 2016
Hydrophobic Interactions Improve Selectivity to ERα for Ben-zothiophene SERMs.ACS medicinal chemistry letters, , Mar-08, Volume: 3, Issue:3, 2012
A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Identification and structure-activity relationships of chromene-derived selective estrogen receptor modulators for treatment of postmenopausal symptoms.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.Journal of medicinal chemistry, , May-31, Volume: 50, Issue:11, 2007
Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 15, Issue:11, 2005
A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 2005
Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 14, Issue:6, 2004
Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators.Journal of medicinal chemistry, , Apr-22, Volume: 47, Issue:9, 2004
Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.Bioorganic & medicinal chemistry letters, , May-17, Volume: 14, Issue:10, 2004
Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
A novel estrogen receptor ligand template.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs).Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 2003
Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor.Bioorganic & medicinal chemistry letters, , Jan-07, Volume: 12, Issue:1, 2002
A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta.Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.Journal of medicinal chemistry, , May-24, Volume: 44, Issue:11, 2001
2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
Novel nonsteroidal selective estrogen receptor modulators. Carbon and heteroatom replacement of oxygen in the ethoxypiperidine region of raloxifene.Bioorganic & medicinal chemistry letters, , Feb-22, Volume: 9, Issue:4, 1999
Synthesis and biological activity of trans-2,3-dihydroraloxifene.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 9, Issue:8, 1999
Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene.Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
Antiestrogens. 3. Estrogen receptor affinities and antiproliferative effects in MCF-7 cells of phenolic analogues of trioxifene, [3,4-dihydro-2-(4- methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]- phenyl]methanone.Journal of medicinal chemistry, , Mar-06, Volume: 35, Issue:5, 1992
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.ACS medicinal chemistry letters, , Apr-09, Volume: 6, Issue:4, 2015
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Synthesis and evaluation of 17α-triazolyl and 9α-cyano derivatives of estradiol.Bioorganic & medicinal chemistry, , 10-01, Volume: 28, Issue:19, 2020
Synthesis and biological evaluation of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors based on a thieno[2,3-d]pyrimidin-4(3H)-one core.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Synthesis and evaluation of 17α-triazolyl and 9α-cyano derivatives of estradiol.Bioorganic & medicinal chemistry, , 10-01, Volume: 28, Issue:19, 2020
Synthesis and evaluation of 17alpha-arylestradiols as ligands for estrogen receptor alpha and beta.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
[no title available]Bioorganic & medicinal chemistry, , 02-01, Volume: 28, Issue:3, 2020
Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERα-selective antagonist.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 23, Issue:14, 2013
Androstene-3,5-dienes as ER-beta selective SERMs.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
Androstenediol analogs as ER-beta-selective SERMs.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 10, Issue:2, 2000
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry, , Jun-15, Volume: 18, Issue:12, 2010
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptors α and β.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen Receptors.Journal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ERα and ERβ Activity.Journal of medicinal chemistry, , 01-25, Volume: 61, Issue:2, 2018
Rational design and optimization of selenophenes with basic side chains as novel potent selective estrogen receptor modulators (SERMs) for breast cancer therapy.MedChemComm, , Jul-01, Volume: 8, Issue:7, 2017
Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.European journal of medicinal chemistry, , Apr-13, Volume: 112, 2016
Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators.Bioorganic & medicinal chemistry, , Nov-01, Volume: 16, Issue:21, 2008
Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Benzothiophene and naphthalene derived constrained SERMs.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 14, Issue:20, 2004
Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs).Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Antiestrogenically active 1,1,2-tris(4-hydroxyphenyl)alkenes without basic side chain: synthesis and biological activity.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 1997
(S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen.Journal of medicinal chemistry, , Jul-04, Volume: 40, Issue:14, 1997
Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene.Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
An overview on Estrogen receptors signaling and its ligands in breast cancer.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Synthesis and characterization of hydrogen peroxide activated estrogen receptor beta ligands.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
A-C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Estrogen Receptor (ER) Subtype Selectivity Identifies 8-Prenylapigenin as an ERβ Agonist from Glycyrrhiza inflata and Highlights the Importance of Chemical and Biological Authentication.Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
Synthesis and structure-activity relationships of 1-benzylindane derivatives as selective agonists for estrogen receptor beta.Bioorganic & medicinal chemistry, , 11-15, Volume: 24, Issue:22, 2016
Diarylpropionitrile (DPN) enantiomers: synthesis and evaluation of estrogen receptor β-selective ligands.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta.European journal of medicinal chemistry, , Volume: 44, Issue:9, 2009
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Discovery of Thieno[2,3-Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
[no title available]Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.Journal of natural products, , Volume: 72, Issue:11, 2009
Design, synthesis, and estrogenic activity of a novel estrogen receptor modulator--a hybrid structure of 17beta-estradiol and vitamin E in hippocampal neurons.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
Synthesis and biological evaluation of stilbene-based pure estrogen antagonists.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 14, Issue:18, 2004
De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 10, Issue:2, 2000
(S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen.Journal of medicinal chemistry, , Jul-04, Volume: 40, Issue:14, 1997
Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
6-(2-adamantan-2-ylidene-hydroxybenzoxazole)-O-sulfamate: a potent non-steroidal irreversible inhibitor of human steroid sulfatase.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.Journal of medicinal chemistry, , May-24, Volume: 44, Issue:11, 2001
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.Journal of medicinal chemistry, , May-31, Volume: 50, Issue:11, 2007
Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Syntheses and biological activities of sulfoximine-based acyclic triaryl olefins.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 22, Issue:13, 2012
De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.Journal of medicinal chemistry, , May-24, Volume: 44, Issue:11, 2001
(S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen.Journal of medicinal chemistry, , Jul-04, Volume: 40, Issue:14, 1997
[no title available]Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Estrogen Receptor (ER) Subtype Selectivity Identifies 8-Prenylapigenin as an ERβ Agonist from Glycyrrhiza inflata and Highlights the Importance of Chemical and Biological Authentication.Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
Subtle side-chain modifications of the hop phytoestrogen 8-prenylnaringenin result in distinct agonist/antagonist activity profiles for estrogen receptors alpha and beta.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Optimisation of estrogen receptor subtype-selectivity of a 4-Aryl-4H-chromene scaffold previously identified by virtual screening.Bioorganic & medicinal chemistry, , 03-01, Volume: 28, Issue:5, 2020
Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ERα and ERβ Activity.Journal of medicinal chemistry, , 01-25, Volume: 61, Issue:2, 2018
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.European journal of medicinal chemistry, , Apr-13, Volume: 112, 2016
β-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Discovery of natural estrogen receptor modulators with structure-based virtual screening.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening.European journal of medicinal chemistry, , Volume: 54, 2012
Hydrophobic Interactions Improve Selectivity to ERα for Ben-zothiophene SERMs.ACS medicinal chemistry letters, , Mar-08, Volume: 3, Issue:3, 2012
Discovery of potent ligands for estrogen receptor beta by structure-based virtual screening.Journal of medicinal chemistry, , Jul-22, Volume: 53, Issue:14, 2010
Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators.Bioorganic & medicinal chemistry, , Nov-01, Volume: 16, Issue:21, 2008
Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells.Journal of medicinal chemistry, , Feb-26, Volume: 47, Issue:5, 2004
Benzoxepin-derived estrogen receptor modulators: a novel molecular scaffold for the estrogen receptor.Journal of medicinal chemistry, , Nov-04, Volume: 47, Issue:23, 2004
Antiestrogenically active 1,1,2-tris(4-hydroxyphenyl)alkenes without basic side chain: synthesis and biological activity.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Flexible estrogen receptor modulators: design, synthesis, and antagonistic effects in human MCF-7 breast cancer cells.Journal of medicinal chemistry, , Mar-29, Volume: 44, Issue:7, 2001
Synthesis and biological activity of trans-2,3-dihydroraloxifene.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 9, Issue:8, 1999
Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 1997
(S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen.Journal of medicinal chemistry, , Jul-04, Volume: 40, Issue:14, 1997
Novel 5-aminoflavone derivatives as specific antitumor agents in breast cancer.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
Constrained phytoestrogens and analogues as ERbeta selective ligands.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
Novel 5-aminoflavone derivatives as specific antitumor agents in breast cancer.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
An overview on Estrogen receptors signaling and its ligands in breast cancer.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Estrogen Receptor (ER) Subtype Selectivity Identifies 8-Prenylapigenin as an ERβ Agonist from Glycyrrhiza inflata and Highlights the Importance of Chemical and Biological Authentication.Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
Design, synthesis, and estrogenic activity of a novel estrogen receptor modulator--a hybrid structure of 17beta-estradiol and vitamin E in hippocampal neurons.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Estrogen receptor beta ligands: design and synthesis of new 2-phenyl-isoindole-1,3-diones.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 17, Issue:1, 2007
Aza analogues of equol: novel ligands for estrogen receptor beta.Bioorganic & medicinal chemistry, , Sep-01, Volume: 15, Issue:17, 2007
ERbeta ligands. Part 5: synthesis and structure-activity relationships of a series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Subtle side-chain modifications of the hop phytoestrogen 8-prenylnaringenin result in distinct agonist/antagonist activity profiles for estrogen receptors alpha and beta.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.Journal of medicinal chemistry, , Jun-16, Volume: 48, Issue:12, 2005
ERbeta ligands. Part 4: Synthesis and structure-activity relationships of a series of 2-phenylquinoline derivatives.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 15, Issue:20, 2005
Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 15, Issue:24, 2005
Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 14, Issue:6, 2004
7-Substituted 2-phenyl-benzofurans as ER beta selective ligands.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 14, Issue:19, 2004
Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
Constrained phytoestrogens and analogues as ERbeta selective ligands.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis.Journal of natural products, , Volume: 65, Issue:12, 2002
Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Novel 5-aminoflavone derivatives as specific antitumor agents in breast cancer.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
[no title available],
Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 14, Issue:6, 2004
An overview on Estrogen receptors signaling and its ligands in breast cancer.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 14, Issue:6, 2004
Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis.Journal of natural products, , Volume: 65, Issue:12, 2002
Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.Bioorganic & medicinal chemistry letters, , Mar-06, Volume: 10, Issue:5, 2000
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 17, Issue:13, 2007
A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 17, Issue:13, 2007
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 4: functionalization of the benzopyran A-ring.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 17, Issue:18, 2007
Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 17, Issue:17, 2007
Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor.Bioorganic & medicinal chemistry letters, , Jan-07, Volume: 12, Issue:1, 2002
Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor.Bioorganic & medicinal chemistry letters, , Feb-21, Volume: 10, Issue:4, 2000
Enables
This protein enables 12 target(s):
Target | Category | Definition |
RNA polymerase II cis-regulatory region sequence-specific DNA binding | molecular function | Binding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site) located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by RNA polymerase II. [GOC:txnOH-2018] |
DNA-binding transcription factor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that modulates the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
nuclear steroid receptor activity | molecular function | Combining with a steroid hormone and transmitting the signal within the cell to initiate a change in cell activity or function. [GOC:signaling, PMID:14708019] |
nuclear receptor activity | molecular function | A DNA-binding transcription factor activity regulated by binding to a ligand that modulates the transcription of specific gene sets transcribed by RNA polymerase II. Nuclear receptor ligands are usually lipid-based (such as a steroid hormone) and the binding of the ligand to its receptor often occurs in the cytosol, which leads to its translocation to the nucleus. [GOC:txnOH-2018, PMID:23457262] |
steroid binding | molecular function | Binding to a steroid, any of a large group of substances that have in common a ring system based on 1,2-cyclopentanoperhydrophenanthrene. [GOC:jl, ISBN:0198506732] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
nuclear estrogen receptor activity | molecular function | Combining with estrogen and transmitting the signal within the cell to trigger a change in cell activity or function. [GOC:signaling, PMID:17615392] |
estrogen response element binding | molecular function | Binding to an estrogen response element (ERE), a conserved sequence found in the promoters of genes whose expression is regulated in response to estrogen. [GOC:ecd, PMID:15036253, PMID:17975005] |
receptor antagonist activity | molecular function | 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] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 1 target(s):
Target | Category | Definition |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
Involved In
This protein is involved in 11 target(s):
Target | Category | Definition |
negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
cell-cell signaling | biological process | Any process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah] |
negative regulation of cell growth | biological process | Any process that stops, prevents, or reduces the frequency, rate, extent or direction of cell growth. [GOC:go_curators] |
intracellular estrogen receptor signaling pathway | biological process | The series of molecular signals initiated by estrogen binding to its nuclear receptor inside the cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling] |
positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
positive regulation of DNA-binding transcription factor activity | biological process | Any process that activates or increases the frequency, rate or extent of activity of a transcription factor, any factor involved in the initiation or regulation of transcription. [GOC:ai] |
cellular response to estradiol stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah] |
regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
cellular response to estrogen stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by an estrogen, C18 steroid hormones that can stimulate the development of female sexual characteristics. [GOC:mah] |