Page last updated: 2024-08-07 15:35:38
Estrogen receptor
An estrogen receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P03372]
Synonyms
ER;
ER-alpha;
Estradiol receptor;
Nuclear receptor subfamily 3 group A member 1
Research
Bioassay Publications (208)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 14 (6.73) | 18.2507 |
2000's | 99 (47.60) | 29.6817 |
2010's | 76 (36.54) | 24.3611 |
2020's | 19 (9.13) | 2.80 |
Compounds (123)
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 |
4-nonylphenol | Homo sapiens (human) | IC50 | 0.3770 | 1 | 0 |
4-nonylphenol | Homo sapiens (human) | Ki | 0.1080 | 1 | 0 |
bicalutamide | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
cyclofenil | Homo sapiens (human) | IC50 | 0.0270 | 1 | 1 |
stallimycin | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
emodin | Homo sapiens (human) | IC50 | 2.7000 | 1 | 1 |
emodin | Homo sapiens (human) | Ki | 0.7700 | 1 | 1 |
letrozole | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
phloretin | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
raloxifene | Homo sapiens (human) | IC50 | 0.0427 | 47 | 49 |
raloxifene | Homo sapiens (human) | Ki | 0.0007 | 9 | 9 |
prednisolone | Homo sapiens (human) | IC50 | 55.0000 | 2 | 2 |
prednisolone | Homo sapiens (human) | Ki | 3.6667 | 3 | 3 |
estriol | Homo sapiens (human) | IC50 | 0.0017 | 1 | 0 |
estriol | Homo sapiens (human) | Ki | 0.0005 | 1 | 0 |
spironolactone | Homo sapiens (human) | IC50 | 12.8510 | 2 | 2 |
spironolactone | Homo sapiens (human) | Ki | 1.1000 | 1 | 1 |
estrone | Homo sapiens (human) | IC50 | 0.1261 | 6 | 6 |
estrone | Homo sapiens (human) | Ki | 0.0022 | 1 | 0 |
ethinyl estradiol | Homo sapiens (human) | IC50 | 0.0035 | 3 | 2 |
ethinyl estradiol | Homo sapiens (human) | Ki | 0.0001 | 1 | 0 |
norethindrone | Homo sapiens (human) | IC50 | 0.8080 | 1 | 0 |
norethindrone | Homo sapiens (human) | Ki | 0.2310 | 1 | 0 |
medroxyprogesterone acetate | Homo sapiens (human) | IC50 | 0.9240 | 2 | 2 |
mestranol | Homo sapiens (human) | IC50 | 0.0180 | 1 | 0 |
mestranol | Homo sapiens (human) | Ki | 0.0052 | 1 | 0 |
3,3'-Dimethylbisphenol A | Homo sapiens (human) | IC50 | 0.8437 | 3 | 3 |
bisphenol a | Homo sapiens (human) | IC50 | 3.4198 | 4 | 3 |
bisphenol a | Homo sapiens (human) | Ki | 0.6490 | 1 | 0 |
2,6-dihydroxyanthraquinone | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
2,6-dihydroxyanthraquinone | Homo sapiens (human) | Ki | 0.3100 | 1 | 1 |
butylparaben | Homo sapiens (human) | IC50 | 1.4200 | 1 | 1 |
androstenediol | Homo sapiens (human) | IC50 | 0.1950 | 2 | 2 |
4-cumylphenol | Homo sapiens (human) | IC50 | 24.0000 | 1 | 1 |
4,4'-bisphenol f | Homo sapiens (human) | IC50 | 5.7135 | 2 | 2 |
ethylestrenol | Homo sapiens (human) | IC50 | 1.1210 | 1 | 0 |
ethylestrenol | Homo sapiens (human) | Ki | 0.3200 | 1 | 0 |
n-butyl gallate | Homo sapiens (human) | IC50 | 8.9700 | 1 | 1 |
4-octylphenol | Homo sapiens (human) | IC50 | 27.6740 | 1 | 0 |
4-octylphenol | Homo sapiens (human) | Ki | 7.9070 | 1 | 0 |
stanozolol | Homo sapiens (human) | IC50 | 0.1130 | 1 | 0 |
stanozolol | Homo sapiens (human) | Ki | 0.0320 | 1 | 0 |
danazol | Homo sapiens (human) | IC50 | 17.7900 | 1 | 0 |
danazol | Homo sapiens (human) | Ki | 5.0830 | 1 | 0 |
levormeloxifene | Homo sapiens (human) | IC50 | 0.0730 | 1 | 1 |
raloxifene hydrochloride | Homo sapiens (human) | IC50 | 0.0053 | 6 | 6 |
mifepristone | Homo sapiens (human) | IC50 | 6.6102 | 8 | 7 |
mifepristone | Homo sapiens (human) | Ki | 6.7385 | 4 | 3 |
octyl gallate | Homo sapiens (human) | IC50 | 8.7400 | 1 | 1 |
1,1-bis(4-hydroxyphenyl)-2-phenylbut-1-ene | Homo sapiens (human) | IC50 | 0.0061 | 3 | 3 |
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol | Homo sapiens (human) | IC50 | 0.4554 | 22 | 22 |
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol | Homo sapiens (human) | Ki | 0.0012 | 8 | 8 |
alfatradiol | Homo sapiens (human) | IC50 | 0.5700 | 1 | 1 |
2,2-bis(4-hydroxyphenyl)-1,1,1-trichloroethane | Homo sapiens (human) | IC50 | 0.0434 | 1 | 1 |
equol | Homo sapiens (human) | IC50 | 5.8760 | 1 | 1 |
anthraglycoside b | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
anthraglycoside b | Homo sapiens (human) | Ki | 5.7000 | 1 | 1 |
effusol | Homo sapiens (human) | IC50 | 0.2400 | 1 | 1 |
fulvestrant | Homo sapiens (human) | IC50 | 0.0061 | 31 | 31 |
fulvestrant | Homo sapiens (human) | Ki | 0.0031 | 3 | 3 |
ici 164384 | Homo sapiens (human) | IC50 | 0.1950 | 2 | 2 |
ici 164384 | Homo sapiens (human) | Ki | 0.0029 | 3 | 3 |
ly 117018 | Homo sapiens (human) | IC50 | 0.1200 | 1 | 1 |
ru 39411 | Homo sapiens (human) | Ki | 0.0415 | 1 | 1 |
zk 119010 | Homo sapiens (human) | IC50 | 0.0470 | 2 | 2 |
bazedoxifene | Homo sapiens (human) | IC50 | 7.9343 | 4 | 4 |
ly 353381 | Homo sapiens (human) | IC50 | 0.0378 | 3 | 4 |
lasofoxifene | Homo sapiens (human) | IC50 | 0.0046 | 8 | 10 |
estradiol 3-benzoate | Homo sapiens (human) | IC50 | 0.0650 | 1 | 0 |
estradiol 3-benzoate | Homo sapiens (human) | Ki | 0.0180 | 1 | 0 |
1,1-bis(4-hydroxyphenyl)cyclohexane | Homo sapiens (human) | IC50 | 0.5200 | 1 | 1 |
4-oxy-6-(4-oxybezoyloxy)dauc-8,9-en | Homo sapiens (human) | IC50 | 0.0331 | 1 | 1 |
naringenin | Homo sapiens (human) | IC50 | 75.3020 | 1 | 1 |
2-methoxyestrone | Homo sapiens (human) | IC50 | 11.0000 | 1 | 1 |
davidigenin | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
eplerenone | Homo sapiens (human) | IC50 | 15.0000 | 2 | 2 |
tibolone | Homo sapiens (human) | IC50 | 0.4333 | 1 | 0 |
tibolone | Homo sapiens (human) | Ki | 0.1238 | 1 | 0 |
fluticasone propionate | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
resveratrol | Homo sapiens (human) | Ki | 0.5797 | 2 | 3 |
diethylstilbestrol | Homo sapiens (human) | IC50 | 0.1312 | 6 | 5 |
diethylstilbestrol | Homo sapiens (human) | Ki | 0.0002 | 5 | 4 |
afimoxifene | Homo sapiens (human) | IC50 | 0.0105 | 14 | 16 |
8-prenylnaringenin | Homo sapiens (human) | IC50 | 0.0625 | 1 | 2 |
8-isopentenylnaringenin | Homo sapiens (human) | IC50 | 0.0570 | 1 | 1 |
1,1-Bis(4-hydroxyphenyl)ethane | Homo sapiens (human) | IC50 | 6.1600 | 1 | 1 |
isoliquiritigenin | Homo sapiens (human) | IC50 | 1.8700 | 1 | 1 |
erb 041 | Homo sapiens (human) | IC50 | 1.2160 | 1 | 1 |
enclomiphene | Homo sapiens (human) | IC50 | 0.0046 | 1 | 0 |
enclomiphene | Homo sapiens (human) | Ki | 0.0013 | 1 | 0 |
tamoxifen citrate | Homo sapiens (human) | IC50 | 1.7000 | 1 | 1 |
tamoxifen | Homo sapiens (human) | IC50 | 1.1796 | 41 | 41 |
tamoxifen | Homo sapiens (human) | Ki | 0.0586 | 4 | 4 |
idoxifene | Homo sapiens (human) | IC50 | 0.0075 | 1 | 1 |
4-hydroxytoremifene | Homo sapiens (human) | IC50 | 0.0070 | 2 | 3 |
N-[2-(2-methyl-1-indolyl)ethyl]benzamide | Homo sapiens (human) | IC50 | 32.7000 | 1 | 0 |
apigenin | Homo sapiens (human) | IC50 | 7.6265 | 2 | 2 |
genistein | Homo sapiens (human) | IC50 | 1.3477 | 23 | 24 |
genistein | Homo sapiens (human) | Ki | 0.2045 | 2 | 1 |
pulmicort | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
coumestrol | Homo sapiens (human) | IC50 | 0.0434 | 2 | 2 |
daidzein | Homo sapiens (human) | IC50 | 175.4267 | 6 | 6 |
daidzein | Homo sapiens (human) | Ki | 1.8000 | 1 | 1 |
caffeic acid phenethyl ester | Homo sapiens (human) | IC50 | 7.9120 | 1 | 0 |
caffeic acid phenethyl ester | Homo sapiens (human) | Ki | 2.2600 | 1 | 0 |
afimoxifene | Homo sapiens (human) | IC50 | 0.0506 | 2 | 2 |
gw 5638 | Homo sapiens (human) | IC50 | 10.9408 | 11 | 11 |
onapristone | Homo sapiens (human) | IC50 | 1.0000 | 2 | 2 |
onapristone | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
broussonin a | Homo sapiens (human) | IC50 | 8.1000 | 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) | Ki | 10.0000 | 2 | 2 |
ly2066948 | Homo sapiens (human) | Ki | 0.0008 | 2 | 3 |
afimoxifene | Homo sapiens (human) | IC50 | 0.0023 | 2 | 2 |
dehydrodiconiferyl alcohol | Homo sapiens (human) | IC50 | 0.0619 | 1 | 1 |
3,4',5-trimethoxystilbene | Homo sapiens (human) | Ki | 0.1766 | 2 | 3 |
way 202196 | Homo sapiens (human) | IC50 | 0.2100 | 1 | 1 |
era-923 | Homo sapiens (human) | IC50 | 0.0078 | 2 | 2 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | IC50 | 33.5000 | 2 | 2 |
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 |
gsk5182 | Homo sapiens (human) | IC50 | 1.0618 | 4 | 5 |
ru 58668 | Homo sapiens (human) | IC50 | 0.0000 | 1 | 1 |
asoprisnil | Homo sapiens (human) | IC50 | 1.9500 | 2 | 2 |
gw 7604 | Homo sapiens (human) | IC50 | 2.3514 | 13 | 13 |
gw 7604 | Homo sapiens (human) | Ki | 0.0025 | 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 |
way-362450 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
4-hydroxy-n-desmethyltamoxifen | Homo sapiens (human) | IC50 | 0.0300 | 1 | 1 |
6-(3-hydroxyphenyl)-2-naphthol | Homo sapiens (human) | IC50 | 0.2300 | 1 | 1 |
erteberel | Homo sapiens (human) | Ki | 0.0019 | 9 | 14 |
ly3201 | Homo sapiens (human) | Ki | 0.0057 | 4 | 6 |
4-(2-phenyl-5,7-bis(trifluoromethyl)pyrazolo(1,5-a)pyrimidin-3-yl)phenol | Homo sapiens (human) | Ki | 1.5277 | 2 | 3 |
ridaifen-b | Homo sapiens (human) | IC50 | 0.0006 | 1 | 1 |
lgd 2226 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
y134 compound | Homo sapiens (human) | IC50 | 0.0003 | 2 | 2 |
moxestrol | Homo sapiens (human) | IC50 | 0.0027 | 2 | 2 |
nitd 609 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
pf-03882845 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
azd9496 | Homo sapiens (human) | IC50 | 0.0004 | 7 | 8 |
way 200070 | Homo sapiens (human) | IC50 | 0.1550 | 1 | 1 |
way-169916 | Homo sapiens (human) | IC50 | 0.6965 | 2 | 2 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
cyclofenil | Homo sapiens (human) | EC50 | 0.0260 | 1 | 1 |
raloxifene | Homo sapiens (human) | EC50 | 0.0149 | 3 | 3 |
spironolactone | Homo sapiens (human) | EC50 | 20.0000 | 1 | 1 |
estrone | Homo sapiens (human) | EC50 | 0.1100 | 6 | 6 |
ethinyl estradiol | Homo sapiens (human) | EC50 | 0.0252 | 2 | 2 |
medroxyprogesterone acetate | Homo sapiens (human) | EC50 | 0.9240 | 1 | 1 |
3,3'-Dimethylbisphenol A | Homo sapiens (human) | EC50 | 5.6910 | 2 | 2 |
bisphenol a | Homo sapiens (human) | EC50 | 3.1940 | 4 | 4 |
ethyl-p-hydroxybenzoate | Homo sapiens (human) | EC50 | 38.2000 | 1 | 1 |
androstenediol | Homo sapiens (human) | EC50 | 0.0260 | 2 | 2 |
4-cumylphenol | Homo sapiens (human) | EC50 | 4.4000 | 1 | 1 |
4,4'-bisphenol f | Homo sapiens (human) | EC50 | 3.9397 | 3 | 3 |
mifepristone | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
1,1-bis(4-hydroxyphenyl)-2-phenylbut-1-ene | Homo sapiens (human) | EC50 | 0.0005 | 2 | 2 |
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol | Homo sapiens (human) | EC50 | 0.0082 | 3 | 3 |
alfatradiol | Homo sapiens (human) | EC50 | 0.2857 | 2 | 2 |
2,2-bis(4-hydroxyphenyl)-1,1,1-trichloroethane | Homo sapiens (human) | EC50 | 0.0307 | 1 | 1 |
2,3-bis(4-hydroxyphenyl)-propionitrile | Homo sapiens (human) | EC50 | 1.6247 | 10 | 10 |
fulvestrant | Homo sapiens (human) | EC50 | 0.0007 | 3 | 3 |
fulvestrant | Homo sapiens (human) | Kd | 0.0047 | 1 | 1 |
estrone-3-o-sulfamate | Homo sapiens (human) | EC50 | 2.6000 | 1 | 1 |
ly 353381 | Homo sapiens (human) | EC50 | 0.0002 | 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 | 0.0025 | 5 | 5 |
8-prenylnaringenin | Homo sapiens (human) | EC50 | 0.0060 | 2 | 2 |
isoxanthohumol | Homo sapiens (human) | EC50 | 1.4000 | 1 | 1 |
1,1-Bis(4-hydroxyphenyl)ethane | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
trans-4-coumaric acid | Homo sapiens (human) | EC50 | 16.1200 | 1 | 1 |
2,4,4'-trihydroxydeoxybenzoin | Homo sapiens (human) | EC50 | 2.0300 | 1 | 1 |
tamoxifen | Homo sapiens (human) | EC50 | 1.1568 | 3 | 5 |
(S)-4',5,7-Trihydroxy-6-prenylflavanone | Homo sapiens (human) | EC50 | 0.4000 | 1 | 1 |
1,3,5-tris(4-hydroxyphenyl)-4-propyl-1h-pyrazole | Homo sapiens (human) | EC50 | 0.0014 | 3 | 3 |
genistein | Homo sapiens (human) | EC50 | 0.9980 | 6 | 6 |
4-hydroxyestradiol | Homo sapiens (human) | EC50 | 0.2857 | 2 | 2 |
gw 5638 | Homo sapiens (human) | EC50 | 0.3900 | 2 | 2 |
broussonin a | Homo sapiens (human) | EC50 | 1.5900 | 1 | 1 |
era-923 | Homo sapiens (human) | EC50 | 0.0001 | 1 | 1 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
gw 7604 | Homo sapiens (human) | EC50 | 0.0017 | 2 | 2 |
licoflavone c | Homo sapiens (human) | EC50 | 0.0500 | 1 | 1 |
erteberel | Homo sapiens (human) | EC50 | 0.0194 | 1 | 1 |
Drugs with Other Measurements
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
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
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
Structural features underlying raloxifene's biophysical interaction with bone matrix.Bioorganic & medicinal chemistry, , 02-15, Volume: 24, Issue:4, 2016
Synthesis and evaluation of raloxifene derivatives as a selective estrogen receptor down-regulator.Bioorganic & medicinal chemistry, , 07-01, Volume: 24, Issue:13, 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
Recent developments in fragment-based drug discovery.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
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
Bioactive compounds from Peperomia pellucida.Journal of natural products, , Volume: 69, Issue:2, 2006
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 15, Issue:11, 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 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 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
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
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
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. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 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 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 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
Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs).Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
A novel estrogen receptor ligand template.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 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
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
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
2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.Journal of medicinal chemistry, , May-24, Volume: 44, Issue:11, 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
[no title available],
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
Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-Journal of medicinal chemistry, , Oct-27, Volume: 54, Issue:20, 2011
Dimethyl-diphenyl-propanamide derivatives as nonsteroidal dissociated glucocorticoid receptor agonists.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
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 novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
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
Structure-based design, synthesis and in vitro characterization of potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 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
[no title available],
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
[no title available],
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
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
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
[no title available]Bioorganic & medicinal chemistry, , 02-01, Volume: 28, Issue:3, 2020
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
Identification of novel estrogen receptor (ER) agonists that have additional and complementary anti-cancer activities via ER-independent mechanism.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 26, Issue:7, 2016
[no title available],
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
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
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
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
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 20, Issue:16, 2010
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry, , Jun-15, Volume: 18, Issue:12, 2010
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry, , Jul-01, Volume: 16, Issue:13, 2008
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
[no title available],
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
Influence of the length and positioning of the antiestrogenic side chain of endoxifen and 4-hydroxytamoxifen on gene activation and growth of estrogen receptor positive cancer cells.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Investigations on estrogen receptor binding. The estrogenic, antiestrogenic, and cytotoxic properties of C2-alkyl-substituted 1,1-bis(4-hydroxyphenyl)-2-phenylethenes.Journal of medicinal chemistry, , Nov-21, Volume: 45, Issue:24, 2002
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.Bioorganic & medicinal chemistry, , 08-15, Volume: 26, Issue:15, 2018
Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
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
Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
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
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.Journal of medicinal chemistry, , 04-13, Volume: 60, 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 and evaluation of tamoxifen derivatives with a long alkyl side chain as selective estrogen receptor down-regulators.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Hydrophobic Interactions Improve Selectivity to ERα for Ben-zothiophene SERMs.ACS medicinal chemistry letters, , Mar-08, Volume: 3, Issue:3, 2012
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
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Isoflavonoids with antiestrogenic activity from Millettia pachycarpa.Journal of natural products, , Volume: 69, Issue:1, 2006
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
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
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 estrogen receptor binding affinities of 7-hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-ones containing a basic side chain.Bioorganic & medicinal chemistry letters, , Apr-17, Volume: 13, 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
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
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
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
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.ACS medicinal chemistry letters, , Jun-11, Volume: 11, Issue:6, 2020
Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.Journal of medicinal chemistry, , 04-12, Volume: 61, Issue:7, 2018
Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.Journal of medicinal chemistry, , 07-27, Volume: 60, Issue:14, 2017
Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD).Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
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
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
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.Bioorganic & medicinal chemistry, , Dec-15, Volume: 23, Issue:24, 2015
(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
Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators.Bioorganic & medicinal chemistry, , 01-01, Volume: 26, Issue:1, 2018
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
Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 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 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 novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 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
Synthesis of a novel fluorescent probe for estrogen receptor.Bioorganic & medicinal chemistry letters, , May-06, Volume: 12, Issue:9, 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],
[no title available]Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Searching for an ideal SERM: Mining tamoxifen structure-activity relationships.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 52, 2021
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.Journal of medicinal chemistry, , 04-12, Volume: 61, Issue:7, 2018
[no title available]ACS medicinal chemistry letters, , Jan-12, Volume: 8, Issue:1, 2017
Design and synthesis of novel selective estrogen receptor degradation inducers based on the diphenylheptane skeleton.MedChemComm, , Jan-01, Volume: 8, Issue:1, 2017
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.Bioorganic & medicinal chemistry, , Dec-15, Volume: 23, Issue:24, 2015
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
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
DESIGNER Extracts as Tools to Balance Estrogenic and Chemopreventive Activities of Botanicals for Women's Health.Journal of natural products, , 08-25, Volume: 80, Issue:8, 2017
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
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Searching for an ideal SERM: Mining tamoxifen structure-activity relationships.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 52, 2021
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
Structure-based drug design, synthesis, In vitro, and In vivo biological evaluation of indole-based biomimetic analogs targeting estrogen receptor-α inhibition.European journal of medicinal chemistry, , Mar-15, Volume: 166, 2019
Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.Journal of medicinal chemistry, , 04-12, Volume: 61, Issue:7, 2018
Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
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
Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Novel SERMs based on 3-aryl-4-aryloxy-2H-chromen-2-one skeleton - A possible way to dual ERα/VEGFR-2 ligands for treatment of breast cancer.European journal of medicinal chemistry, , Nov-10, Volume: 140, 2017
Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.European journal of medicinal chemistry, , Apr-13, Volume: 112, 2016
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
β-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
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
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.Bioorganic & medicinal chemistry, , Aug-01, Volume: 18, Issue:15, 2010
Discovery of potent ligands for estrogen receptor beta by structure-based virtual screening.Journal of medicinal chemistry, , Jul-22, Volume: 53, Issue:14, 2010
N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 19, Issue:4, 2009
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
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
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
Investigations on estrogen receptor binding. The estrogenic, antiestrogenic, and cytotoxic properties of C2-alkyl-substituted 1,1-bis(4-hydroxyphenyl)-2-phenylethenes.Journal of medicinal chemistry, , Nov-21, Volume: 45, Issue:24, 2002
Synthesis of a novel fluorescent probe for estrogen receptor.Bioorganic & medicinal chemistry letters, , May-06, Volume: 12, Issue:9, 2002
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
Carboxylic acid analogues of tamoxifen: (Z)-2-[p-(1, 2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine. Estrogen receptor affinity and estrogen antagonist effects in MCF-7 cells.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
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
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
Influence of chlorine or fluorine substitution on the estrogenic properties of 1-alkyl-2,3,5-tris(4-hydroxyphenyl)-1H-pyrroles.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
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
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
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
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
Aza analogues of equol: novel ligands for estrogen receptor beta.Bioorganic & medicinal chemistry, , Sep-01, Volume: 15, Issue:17, 2007
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
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
Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 15, Issue:24, 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
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
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
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
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
7-Substituted 2-phenyl-benzofurans as ER beta selective ligands.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 14, Issue:19, 2004
Constrained phytoestrogens and analogues as ERbeta selective ligands.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 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
Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis.Journal of natural products, , Volume: 65, Issue:12, 2002
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
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
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
Effects of 7-O substitutions on estrogenic and anti-estrogenic activities of daidzein analogues in MCF-7 breast cancer cells.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
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
Estrogen signaling: An emanating therapeutic target for breast cancer treatment.European journal of medicinal chemistry, , Sep-01, Volume: 177, 2019
Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
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
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 10, Issue:2, 2000
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
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
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.Journal of medicinal chemistry, , May-24, Volume: 44, Issue:11, 2001
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.MedChemComm, , Aug-01, Volume: 10, Issue:8, 2019
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.European journal of medicinal chemistry, , Nov-01, Volume: 205, 2020
Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.Journal of medicinal chemistry, , 11-23, Volume: 59, Issue:22, 2016
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Estrogen signaling: An emanating therapeutic target for breast cancer treatment.European journal of medicinal chemistry, , Sep-01, Volume: 177, 2019
Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
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
Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 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 4: functionalization of the benzopyran A-ring.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 17, Issue:18, 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 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 5: Combined A- and C-ring structure-activity relationship studies.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 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 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 5: Combined A- and C-ring structure-activity relationship studies.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 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
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
Design, syntheses and evaluations of novel indole derivatives as orally selective estrogen receptor degraders (SERD).Bioorganic & medicinal chemistry letters, , 11-15, Volume: 30, Issue:22, 2020
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.ACS medicinal chemistry letters, , Oct-10, Volume: 10, Issue:10, 2019
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Enables
This protein enables 26 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] |
TFIIB-class transcription factor binding | molecular function | Binding to a general RNA polymerase II transcription factor of the TFIIB class, one of the factors involved in formation of the preinitiation complex (PIC) by RNA polymerase II. [GOC:krc, PMID:16858867] |
transcription coregulator binding | molecular function | Binding to a transcription coregulator, a protein involved in regulation of transcription via protein-protein interactions with transcription factors and other transcription regulatory proteins. Cofactors do not bind DNA directly, but rather mediate protein-protein interactions between regulatory transcription factors and the basal transcription machinery. [GOC:krc] |
transcription corepressor binding | molecular function | Binding to a transcription corepressor, a protein involved in negative regulation of transcription via protein-protein interactions with transcription factors and other proteins that negatively regulate transcription. Transcription corepressors do not bind DNA directly, but rather mediate protein-protein interactions between repressing transcription factors and the basal transcription machinery. [GOC:krc] |
transcription coactivator binding | molecular function | Binding to a transcription coactivator, a protein involved in positive regulation of transcription via protein-protein interactions with transcription factors and other proteins that positively regulate transcription. Transcription coactivators do not bind DNA directly, but rather mediate protein-protein interactions between activating transcription factors and the basal transcription machinery. [GOC:krc] |
DNA-binding transcription activator activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that activates or increases transcription of specific gene sets transcribed by RNA polymerase II. [GOC:aruk, GOC:txnOH-2018, PMID:20737563, PMID:27145859] |
chromatin binding | molecular function | Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130] |
DNA-binding transcription factor activity | molecular function | A transcription regulator activity that modulates transcription of gene sets via selective and non-covalent binding to a specific double-stranded genomic DNA sequence (sometimes referred to as a motif) within a cis-regulatory region. Regulatory regions include promoters (proximal and distal) and enhancers. Genes are transcriptional units, and include bacterial operons. [GOC:txnOH-2018] |
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] |
calmodulin binding | molecular function | Binding to calmodulin, a calcium-binding protein with many roles, both in the calcium-bound and calcium-free states. [GOC:krc] |
beta-catenin binding | molecular function | Binding to a catenin beta subunit. [GOC:bf] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
TBP-class protein binding | molecular function | Binding to a member of the class of TATA-binding proteins (TBP), including any of the TBP-related factors (TRFs). [GOC:jl, GOC:txnOH, http://www.mblab.gla.ac.uk/, PMID:16858867] |
enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
nitric-oxide synthase regulator activity | molecular function | Binds to and modulates the activity of nitric oxide synthase. [GOC:mah] |
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] |
nuclear estrogen receptor binding | molecular function | Binding to a nuclear estrogen receptor. [GOC:ai] |
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] |
identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
ATPase binding | molecular function | Binding to an ATPase, any enzyme that catalyzes the hydrolysis of ATP. [GOC:ai] |
14-3-3 protein binding | molecular function | Binding to a 14-3-3 protein. A 14-3-3 protein is any of a large family of approximately 30kDa acidic proteins which exist primarily as homo- and heterodimers within all eukaryotic cells, and have been implicated in the modulation of distinct biological processes by binding to specific phosphorylated sites on diverse target proteins, thereby forcing conformational changes or influencing interactions between their targets and other molecules. Each 14-3-3 protein sequence can be roughly divided into three sections: a divergent amino terminus, the conserved core region and a divergent carboxy-terminus. The conserved middle core region of the 14-3-3s encodes an amphipathic groove that forms the main functional domain, a cradle for interacting with client proteins. [GOC:cna, GOC:mah, PMID:15167810, PMID:19575580] |
sequence-specific double-stranded DNA binding | molecular function | Binding to double-stranded DNA of a specific nucleotide composition, e.g. GC-rich DNA binding, or with a specific sequence motif or type of DNA, e.g. promotor binding or rDNA binding. [GOC:dos, GOC:sl] |
Located In
This protein is located in 7 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] |
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
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 4 target(s):
Target | Category | Definition |
transcription regulator complex | cellular component | A protein complex that is capable of associating with DNA by direct binding, or via other DNA-binding proteins or complexes, and regulating transcription. [GOC:jl] |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
euchromatin | cellular component | A dispersed and relatively uncompacted form of chromatin that is in a transcription-competent conformation. [PMID:32017156] |
protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
Involved In
This protein is involved in 42 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] |
antral ovarian follicle growth | biological process | Increase in size of antral follicles due to cell proliferation and/or growth of the antral cavity. [https://www.ncbi.nlm.nih.gov/books/NBK279054/] |
epithelial cell development | biological process | The process whose specific outcome is the progression of an epithelial cell over time, from its formation to the mature structure. An epithelial cell is a cell usually found in a two-dimensional sheet with a free surface. [GOC:dph] |
chromatin remodeling | biological process | A dynamic process of chromatin reorganization resulting in changes to chromatin structure. These changes allow DNA metabolic processes such as transcriptional regulation, DNA recombination, DNA repair, and DNA replication. [GOC:jid, GOC:vw, PMID:12042764, PMID:12697820] |
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] |
phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
androgen metabolic process | biological process | The chemical reactions and pathways involving androgens, C19 steroid hormones that can stimulate the development of male sexual characteristics. [ISBN:0198506732] |
male gonad development | biological process | The process whose specific outcome is the progression of the male gonad over time, from its formation to the mature structure. [GOC:jid] |
negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
positive regulation of phospholipase C activity | biological process | Any process that increases the rate of phospholipase C activity. [GOC:dph, GOC:tb] |
intracellular steroid hormone receptor signaling pathway | biological process | The series of molecular signals initiated by a steroid binding to an intracellular steroid hormone receptor. [GOC:mah, GOC:signaling] |
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] |
response to estradiol | biological process | Any process that results in a change in state or activity of a cell or an organism (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, ISBN:0911910123] |
regulation of toll-like receptor signaling pathway | biological process | Any process that modulates the frequency, rate, or extent of toll-like receptor signaling pathway. [GOC:add, PMID:16551253, PMID:17328678] |
negative regulation of smooth muscle cell apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of smooth muscle cell apoptotic process. [GOC:BHF, GOC:mtg_apoptosis, GOC:rl] |
negative regulation of canonical NF-kappaB signal transduction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl] |
negative regulation of DNA-binding transcription factor activity | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the activity of a transcription factor, any factor involved in the initiation or regulation of transcription. [GOC:jl] |
response to estrogen | biological process | Any process that results in a change in state or activity of a cell or an organism (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:jl, ISBN:0198506732] |
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 transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
fibroblast proliferation | biological process | The multiplication or reproduction of fibroblast cells, resulting in the expansion of the fibroblast population. [GOC:jid] |
positive regulation of fibroblast proliferation | biological process | Any process that activates or increases the frequency, rate or extent of multiplication or reproduction of fibroblast cells. [GOC:jid] |
stem cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a stem cell. A stem cell is a cell that retains the ability to divide and proliferate throughout life to provide progenitor cells that can differentiate into specialized cells. [CL:0000034, GOC:isa_complete] |
regulation of inflammatory response | biological process | Any process that modulates the frequency, rate or extent of the inflammatory response, the immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. [GOC:ai] |
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] |
RNA polymerase II preinitiation complex assembly | biological process | The formation of a large multiprotein-DNA complex that self-assembles on gene promoter through the sequential recruitment of the general initiation factors that compose the preinitiation complex (PIC) (which may include TFIIA, TFIIB, TFIID, TFIIE, TFIIF, and TFIIH complexes). The PIC engages RNA polymerase II on its DNA template strand and sparks polymerization of the first few RNA nucleotides of the nascent transcript, of which 8 are base-paired with the DNA template within a DNA bubble. PIC assembly may result in a pause step, which marks the end of the PIC assembly and may be followed by promoter clearance (exact synonym: promoter escape). For RNA polymerase II PIC assembly is preceded by the formation of a nucleosome-free region that allows the transcription machinery to access the promoter DNA. [GOC:txnOH, PMID:15020047, PMID:31300188] |
uterus development | biological process | The reproductive developmental process whose specific outcome is the progression of the uterus over time, from its formation to the mature structure. [GOC:dph, GOC:ebc] |
vagina development | biological process | The reproductive developmental process whose specific outcome is the progression of the vagina over time, from its formation to the mature structure. [GOC:dph, GOC:ebc] |
prostate epithelial cord elongation | biological process | The developmental growth process in which solid chords of prostate epithelium increase in length. [GOC:dph, PMID:18977204] |
prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis | biological process | The branching morphogenesis process in which the prostate epithelial cords branch freely to create the structure of the prostate acini. [GOC:dph, PMID:18977204] |
regulation of branching involved in prostate gland morphogenesis | biological process | Any process that modulates the rate, frequency, or extent of prostate gland branching, the process in which the branching structure of the prostate gland is generated and organized. A branch is a division or offshoot from a main stem. [GOC:dph] |
mammary gland branching involved in pregnancy | biological process | The process in which the branching structure of the mammary gland duct is generated and organized as a part of pregnancy. [GOC:dph, PMID:19261859] |
mammary gland alveolus development | biological process | The progression of the mammary gland alveolus over time, from its formation to its mature state. The mammary gland alveolus is a sac-like structure that is found in the mature gland. [GOC:dph] |
epithelial cell proliferation involved in mammary gland duct elongation | biological process | The multiplication or reproduction of mammary gland branch epithelial cells, resulting in the elongation of the branch. The mammary gland branch differs from the bud in that it is not the initial curved portion of the outgrowth. [GOC:dph] |
protein localization to chromatin | biological process | Any process in which a protein is transported to, or maintained at, a part of a chromosome that is organized into chromatin. [GOC:mah] |
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] |
negative regulation of miRNA transcription | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of microRNA (miRNA) gene transcription. [GO_REF:0000058, GOC:dph, GOC:kmv, GOC:TermGenie, PMID:24699545] |
regulation of epithelial cell apoptotic process | biological process | Any process that modulates the frequency, rate or extent of epithelial cell apoptotic process. [GO_REF:0000058, GOC:TermGenie, PMID:19137015] |
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] |