| S8686 |
PHTPP |
PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα. |
Selective |
|
| S3929 |
Liquiritigenin |
Liquiritigenin (4',7-Dihydroxyflavanone), the most active estrogenic compound from the root of Glycyrrhizae uralensis Fisch, selectively binds to ERβ with an IC50 value of 7.5 μM and activates multiple ER regulatory elements and native target genes with Erβ but not ERα. |
Selective |
|
| S4418 |
Phenol Red sodium salt |
Phenol Red sodium salt (Phenolsulfonephthalein sodium salt) is used ubiquitously as a pH indicator in tissue culture media ranging from 6.8 (yellow) to 8.2 (red). Phenol red binds to the estrogen receptor of MCF-7 human breast cancer cells. |
Selective |
|
| S8372 |
AZD9496 |
AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models. |
Selective |
|
| S9862 |
ARV471 |
ARV471 is an orally bioavailable estrogen receptor-targeting (ER-targeting) PROTAC for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer. |
Selective |
|
| S4629 |
Chlorotrianisene |
Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator. |
Selective |
|
| S8958 |
Camizestrant (AZD9833) |
Camizestrant (AZD9833) is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity. |
Selective |
|
| S2473 |
Hexestrol |
Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively. |
Selective |
ERα, EC50: 0.07 nM; ERβ, EC50: 0.175 nM |
| S9609 |
Amcenestrant (SAR439859) |
Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation. |
Selective |
ERα, EC50: 0.2 nM |
| S8746 |
H3B-5942 |
H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively. |
Selective |
ERα WT, Ki: 1 nM; ERα (Y537S), Ki: 0.41 nM |
| S6810 |
Diarylpropionitrile (DPN) |
Diarylpropionitrile (DPN) is a non-steroidal estrogen receptor β (ERβ) agonist with EC50 of 0.85 nM, 72-fold more selective for ERβ than ERα. |
Selective |
estrogen receptor β, EC50: 0.85 nM |
| S1191 |
Fulvestrant |
Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity. |
Selective |
ER, IC50: 0.94 nM |
| S9520 |
Lasofoxifene Tartrate |
Lasofoxifene Tartrate is a third-generation, non-steroidal selective estrogen receptor modulator (SERM) which binds with high affinity to the human estrogen receptor-α with IC50 value of 1.5 nM. |
Selective |
estrogen receptor, IC50: 1.5 nM |
| S4110 |
Estradiol Benzoate |
Estradiol benzoate(β-Estradiol 3-benzoate) is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM. |
Selective |
hERα, IC50: 28 nM; mERα, IC50: 2.3 nM |
| S5781 |
Raloxifene |
Raloxifene (Keoxifene, Pharoxifene, LY-139481, LY-156758, CCRIS-7129) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. |
Selective |
ER, IC50: 5.7 nM |
| S1227 |
Raloxifene HCl |
Raloxifene (LY156758, Keoxifene) HCl is a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM. |
Selective |
ER, IC50: 5.7 nM |
| S7855 |
Brilanestrant (GDC-0810) |
Brilanestrant (GDC-0810, ARN-810） is a potent ER-α binder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors. |
Selective |
ERα, IC50: 6.1 nM; ERβ, IC50: 8.8 nM |
| S0851 |
G-1 |
G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM. |
Selective |
GPR30, Ki: 11 nM |
| S2128 |
Bazedoxifene (WAY-140424) HCl |
Bazedoxifene HCl (WAY-140424, TSE-424) is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively. |
Selective |
ERα, IC50: 23 nM; ERβ, IC50: 89 nM |
| S9629 |
Elacestrant (RAD1901) Dihydrochloride |
Elacestrant (RAD1901) Dihydrochloride is an orally available selective estrogen receptor degrader (SERD) with IC50 of 48 nM and 870 nM for ERα and ERβ, respectively. |
Selective |
ERα, IC50: 48 nM; ERβ, IC50: 870 nM |
| S5676 |
Zearalenone |
Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER). |
Selective |
ERα, IC50: 240.4 nM; ERβ, IC50: 165.7 nM |
| S5464 |
Psoralidin |
Psoralidin, a naturally occurring coumestan isolated from the fractions of organic solvents such as ethylacetate, hexane, or n-butanol of the seed extract of Psoralea corylifolia L., has a variety of biological activities such as anticancer, antioxidant, antibacterial, antidepressant, anti-inflammatory activities, and regulation of insulin signaling. It is an agonist for both estrogen receptor (ER)α and ERβ with binding affinities (IC50s) of 1.03 and 24.6 μM, respectively. |
Selective |
ERα, IC50: 1.03 μM; ERβ, IC50: 24.6 μM |
| S6651 |
G15 (GRB-G15) |
G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM. |
Selective |
|
| S4046 |
Estradiol Cypionate |
Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor. |
Selective |
|
| S2450 |
Equol |
Equol ,a metabolite of soybeans, is an important isoflavone in humans，specifically binds to 5α-DHT, has a modest affinity for recombinant estrogen receptor ERβ. Phase 2. |
Selective |
|
| S1776 |
Toremifene Citrate (NK 622) |
Toremifene Citrate (NK 622, NSC 613680) is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer. |
Selective |
|
| S1859 |
Diethylstilbestrol |
Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications. |
Selective |
|
| S1238 |
Tamoxifen |
Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. |
Selective |
|
| S3149 |
Estradiol valerate |
Estradiol(E2V) is a synthetic ester used to treat menopausal symptoms and hormone deficiencies. |
Selective |
|
| S1665 |
Estrone |
Estrone is an estrogenic hormone. |
Selective |
|
| S1972 |
Tamoxifen (ICI 46474) Citrate |
Tamoxifen Citrate (Istubal,ICI 46474 Citrate) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy. |
Selective |
|
| S7839 |
Endoxifen HCl |
Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
|
Selective |
|
| S4285 |
Ospemifene |
Ospemifene(FC-1271a) is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.
|
Selective |
|
| S1625 |
Ethinyl Estradiol |
Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. |
Selective |
|
| S1709 |
Estradiol |
Estradiol (17β-estradiol, β-Estradiol, E2, 17β-Oestradiol) is a human sex hormone and steroid, and the primary female sex hormone. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway. |
Selective |
|
| S2125 |
Mestranol |
Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives. |
Selective |
|
| S2466 |
Estriol |
Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells. |
Selective |
|
| S2561 |
Clomifene citrate |
Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction. |
Selective |
|
| S4440 |
2-Phenylacetamide |
2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells. |
Selective |
|
| S5393 |
Cyclofenil |
Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα. |
Selective |
|
| S2167 |
Bazedoxifene (TSE-424) acetate |
Bazedoxifene Acetate (WAY-140424,TSE-424 acetate) is a third generation selective estrogen receptor modulator (SERM). |
Selective |
|
| S0503 |
Estrogen receptor modulator 1 |
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM) with pIC50 of 0.46. Estrogen receptor modulator 1 exhibits potential anti-tumor activity. |
Selective |
ER, pIC50: 0.46 |
