Home Endocrinology & Hormones Estrogen/progestogen Receptor

Estrogen/progestogen Receptor

Isoform-selective Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathway

Estrogen/progestogen Receptor Products

  • All (102)
  • Estrogen/progestogen Receptor Inhibitors (4)
  • Estrogen/progestogen Receptor Activators (3)
  • Estrogen/progestogen Receptor Antagonists (15)
  • Estrogen/progestogen Receptor Agonists (45)
  • Estrogen/progestogen Receptor Modulators (24)
  • New Estrogen/progestogen Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
Cancer Lett, 2024, 593:216968
Cell Death Dis, 2024, 15(8):590
Cell Death Dis, 2024, 15(7):480
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.
Nat Commun, 2024, 15(1):2377
Breast Cancer Res, 2024, 26(1):33
Toxics, 2024, 12(4)247
S2606 Mifepristone Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Neuron, 2024, S0896-6273(24)00089-8
Cell Death Dis, 2024, 15(1):70
Cell Death Dis, 2024, 15(1):73
S7827 4-Hydroxytamoxifen (Afimoxifene) 4-Hydroxytamoxifen (Afimoxifene) is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.
Nat Commun, 2024, 15(1):2983
Cell Rep Med, 2024, 5(3):101468
Cell Rep, 2024, S2211-1247(23)01591-7
S1972 Tamoxifen Citrate Tamoxifen 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.
bioRxiv, 2024, 2023.05.10.540211
RNA, 2023, 29(9):1325-1338.
RNA, 2023, rna.079509.122
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.
iScience, 2024, 27(3):109125
Eur J Immunol, 2024, e2451226.
Pharmaceuticals (Basel), 2024, 17(3)388
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.
Cell Death Dis, 2024, 15(4):255
Int J Mol Sci, 2023, 24(4)3356
Cells, 2022, 11(3)381
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.
Viruses, 2024, 16(8)1332
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2561 Clomifene citrate Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S2567 MPA (Medroxyprogesterone acetate) MPA (Medroxyprogesterone acetate) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.
J Transl Med, 2024, 22(1):478
Hepatol Commun, 2024, 8(5)e0437
Cancer Rep (Hoboken), 2024, 7(1):e1934
S1304 Megestrol Acetate Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S4154 Cholesterol Cholesterol(Cholesterin) is the principal sterol of all higher animals required to build and maintain membranes.
Clin Transl Med, 2023, 13(9):e1415
Clin Transl Med, 2023, 13(9):e1415
Biol Proced Online, 2023, 25(1):31
S1705 Progesterone Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.
Nat Commun, 2024, 15(1):8708
Dev Cell, 2024, S1534-5807(24)00326-5
Mol Med, 2024, 30(1):123
S1859 Diethylstilbestrol Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.
Biomater Res, 2024, 28:0010
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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.
Viruses, 2024, 16(4)640
Endocrinology, 2021, 162(10)bqab142
bioRxiv, 2020, 2020/9/20.4.7.30734
S7839 Endoxifen HCl Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Viruses, 2024, 16(8)1332
Blood Cancer J, 2022, 12(3):36
J Mol Cell Biol, 2021, mjab018
S2167 Bazedoxifene acetate Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM).
Viruses, 2024, 16(8)1332
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Transl Oncol, 2021, 14(11):101192
S6651 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.
iScience, 2024, 27(3):109125
Nutrients, 2023, 16(1)38
Chem Biol Interact, 2023, 10.1016/j.cbi.2023.110728
S7828 Licochalcone A Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.
Br J Pharmacol, 2023, 180(8):1114-1131
Eur J Pharmacol, 2023, 957:176031
Front Oncol, 2022, 12:1006131
S1727 Levonorgestrel Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation.
Pharmaceuticals -Basel, 2022, 15-101226
J Control Release, 2021, S0168-3659(21)00550-2
Nat Cancer, 2020, 1(2):235-248
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.
Neural Plast, 2023, 2023:5225952
Front Pharmacol, 2022, 13:841941
Nutr Metab (Lond), 2021, 18(1):63
S8372 AZD9496 AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.
Breast Cancer Res, 2023, 25(1):96
Breast Cancer Res, 2023, 25(1):96
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
S8686 PHTPP PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.
J Cancer, 2022, 13(5):1573-1587
Brain Res, 2021, 1768:147580
Ecotoxicol Environ Saf, 2020, 208:111429
S1377 Drospirenone Drospirenone (ZK 3059) is a synthetic progestin that is an analog to spironolactone.
Nat Cancer, 2020, 1(2):235-248
J Thromb Haemost, 2015, 13(10):1918-24
S3081 Ulipristal Acetate (CDB 2914) Ulipristal acetate (CDB-2914, HRP 2000, RU 44675) is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.
J Clin Endocrinol Metab, 2019, 104(12):6256-6264
Cell Prolif, 2017, 50(5)
S1625 Ethinyl Estradiol Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
Hum Mol Genet, 2020, ddaa244
Regul Toxicol Pharmacol, 2020, S0273-2300(20)30246-4
S1914 Pregnenolone Pregnenolone(3β-Hydroxy-5-pregnen-20-one) is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.
Cells, 2024, 13(19)1622
Biol Proced Online, 2023, 25(1):31
J Sep Sci, 2019, 42(10):1833-1841
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.
Chin Med, 2024, 19(1):12
Mol Med Rep, 2021, 24(4)686
Mol Med Rep, 2021, 24(4)686
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.
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
Nat Genet, 2019, 51(2):207-216
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.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Drug Test Anal, 2020, 10.1002/dta.2917
S4673 Etonogestrel Etonogestrel (Implanon, Nexplanon, 3-Oxodesogestrel, 3-keto-Desogestrel) is a synthetic form of the naturally occurring female sex hormone progesterone. It binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression.
Pharmaceutics, 2024, 16(8)1030
Biomaterials, 2023, 301:122260
Breast Cancer Res, 2023, 25(1):75
S1598New Erteberel (LY500307) LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.
University of North Texas, 2014, Health Science Center at Fort Worth
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.
ACS Chem Biol, 2015, 10.1021/cb5009487
S2466 Estriol Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Mol Cell, 2019, 75(6):1103-1116.e9
S3149 Estradiol valerate Estradiol(E2V) is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.
Front Immunol, 2022, 13:1026214
S1665 Estrone Estrone is an estrogenic hormone.
Mol Cell, 2019, 75(6):1103-1116.e9
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.
Mol Cancer Res, 2021, 19(6):1026-1039
S4046 Estradiol Cypionate Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.
Nat Commun, 2024, 15(1):4549
Cell Death Dis, 2024, 15(8):590
Cell Commun Signal, 2024, 22(1):195
S2301 Genistin (Genistoside) Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway.
Acta Biomater, 2021, S1742-7061(21)00586-9
S8956 (Z)-4-Hydroxytamoxifen (Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor.
iScience, 2024, 27(3):109125
Toxicol Sci, 2023, kfad049
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.
Front Oncol, 2022, 12:857590
S3449 GSK5182 GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.
Nat Genet, 2023, 55(2):187-197
S1251 Dienogest Dienogest (STS 557) is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.
S1376 Gestodene Gestodene (SH B 331,WL 70) is a progestogen hormonal contraceptive.
S2473 Hexestrol Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.
S2125 Mestranol Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.
S3167 Altrenogest Altrenogest (A35957, RU2267,R2267) is a progestogen structurally related to veterinary steroid trenbolone.
E0527 Norgestimate Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity.
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.
S5872 Estradiol dipropionate Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a semisynthetic, steroidal estrogen which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders.
Pharmaceuticals (Basel), 2022, 16(1)25
S3617 (20S)-Protopanaxatriol (20S)-Protopanaxatriol (g-PPT, 20(S)-APPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta and could modulate endothelial cell functions through the glucocorticoid receptor (GR) and estrogen receptor (ER).
S9207 Gypenoside XVII Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.GP-17 treatment predominantly up-regulating the expression of ERα but not ERβ.
E1301New Imlunestrant Imlunestrant(LY3484356) is a potent, orally bioavailable selective estrogen receptor degrader (SERD) that functions as a pure antagonist of estrogen receptor alpha (ERα). It inhibits ER-dependent gene transcription and cell proliferation, resulting in sustained suppression of estrogen-driven growth in ER-positive cells.
S6927 Dihydroresveratrol Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator.
E0937 Segesterone acetate Segesterone acetate (Nestoron, ST-1435) is a synthetic progestin that binds to the progesterone receptor with EC50 of 50.3 nM.
E4845New Ulipristal Ulipristal(Deacetyl CDB-2914, CDB-3236) is a selective modulator of progesterone receptors used in a single dose as an emergency postcoital contraceptive.
S6601 (±)-Equol (±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein.
E0532 Menotropin Menotropin (Human Menopausal Gonadotrophin) is a hormonally active medication for the treatment of fertility disturbances, which are extracted from the urine of postmenopausal women.
E0361 Enclomiphene Citrate

Enclomiphene citrate is the trans isomer of clomiphene citrate and acts as a non-steroidal estrogen receptor antagonist.
S4629 Chlorotrianisene Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.
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.
Biomater Res, 2024, 28:0010
S5676 Zearalenone Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER).
E1903New SLU-PP-332 SLU-PP-332 is an agonist of pan-Estrogen Receptor/ERR with EC50 values of 98nM, 230nM, and 430 nM for ERRα, ERRβ, and ERRγ, respectively with the highest potency for ERRα. SLUPP-332 amplifies mitochondrial function and cellular respiration in skeletal muscle cell lines and also offers opportunities for researching metabolic ailments and enhancing muscle functionality.
S5288 Estropipate Estropipate (Piperazine estrone sulfate, Estrone sulfate piperazine salt, Pipestrone) is a natural estrogenic substance composed of estrone sulfate and piperazine and is used mainly in menopausal hormone therapy in the treatment of menopausal symptoms.
S9862 Vepdegestrant (ARV471) Vepdegestrant (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.
E0940 Propyl pyrazole triol (PPT) Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist.
S5738 Megestrol Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.
S5785 Norethindrone acetate Norethindrone acetate (19-Norethindrone acetate, NA) is a common synthetic hormone used in oral contraceptives. Norethindrone acetate is a well-tolerated, effective option to manage pain and bleeding for all stages of endometriosis.
S4638 Desogestrel Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.
S0358 GSK4716 GSK4716 is a selective agonist of Estrogen-Related Orphan Nuclear Receptors ERR and ERRγ with an IC50 of 2 µM in the ERRγ FRET assay.
S8687New MPP dihydrochloride Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein's interaction with ERα.
S3657 Promestriene Promestriene (3-propyl ethyl, 17B-methyl estradiol) is a synthetic estrogen analog that has been reported to significantly improve the symptoms of vaginal atrophy caused by estrogen deprivation in topical application.
S2314 Kaempferol Kaempferol, a natural flavonol, functions as an ERRα and ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation and may also inhibit the activity of fatty acid synthase.
Int J Mol Sci, 2023, 24(19)14519
Front Pharmacol, 2023, 14:1047184
Front Pharmacol, 2023, 14:1047184
S5219 Allylestrenol Allylestrenol is an orally active progestagen of the 19-nortestosterone series resembling progesterone.
S1858 Dienestrol Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist.
Biomater Res, 2024, 28:0010
S4883 Lynestrenol Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity.
E0707 Nomegestrol Acetate Nomegestrol Acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.
S3635 Medroxyprogesterone Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist.
S4674 Hydroxyprogesterone caproate Hydroxyprogesterone Caproate (17α-Hydroxyprogesterone hexanoate, 17α-Hydroxyprogesterone caproate) is a synthetic progestational agent. It binds to and activates nuclear progesterone receptors in the reproductive system and inhibits ovulation and an alteration in the cervical mucus and endometrium.
Nat Commun, 2024, 15(1):8708
S0143 WAY-200070 WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM.
S3671 Quinestrol Quinestrol (Ethinylestradiol 3-cyclopentyl ether, EE2CPE, W-3566) is a synthetic, steroidal estrogen which is used in hormone replacement therapy and occasionally to treat breast cancer and prostate cancer.
S8958 Camizestrant (AZD9833) Camizestrant (AZD9833) is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.
Viruses, 2024, 16(8)1332
S4097 Dydrogesterone Dydrogesterone (NSC 92336) is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus.
S0407 XCT790 XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis.
S5910 Alpha-Estradiol Alpha-Estradiol (α-Estradiol, 17 alpha-Estradiol, Alfatradiol, Epiestradiol, Epiestrol, Alora, 17 α-E2), a natural, non-feminizing stereoisomer, a hormonally almost inactive isomer of physiological 17 beta-estradiol (17 β-E2), is a weak inhibitor of estrogen.
Biomater Res, 2024, 28:0010
S5364 DY131 DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).
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.
S0851 G-1 (LNS 8801) 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.
iScience, 2024, 27(3):109125
S4507 17-Hydroxyprogesterone 17-Hydroxyprogesterone (17-OHP) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
S9122 Tectorigenin Tectorigenin (TEC) is an isoflavone isolated from various medicinal plants, such as Pueraria thunbergiana Benth, Belamcanda chinensis, and Iris unguicularis. It has been reported to exert pharmacological actions, including antitumor and antibacterial effects, free radical neutralization, and selective estrogen receptor modulation.
E2401 SPP-86 SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
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.
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.
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.
E1842New Palazestrant Palazestrant(OP-1250) is an orally bioavailable complete antagonist of estrogen receptor (ER) that blocks ER activity. It exhibits antiproliferative and antitumor activity in ER-positive (ER+) breast cancer models.
S3160 Ethynodiol diacetate Ethynodiol diacetate (8080 CB,Ethynodiol acetate) is one of the first synthetic progestogens used in contraceptive pills.
E4947New Estrone sulfate sodium Estrone sulfate (Estrone 3-sulfate sodium salt, Premarin), an inactive form of estrogen, serves as a major circulating estrogen in the plasma. It is converted into the active form, estrone (E1), through the action of steroid sulfatase (STS. Estrone sulfate is commonly used in breast cancer research.
S4285 Ospemifene Ospemifene(FC-1271a) is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.
S2611 Ethisterone Ethisterone(17α-Ethynyltestosterone) is a progestogen hormone being considered to treat prostate cancer.
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.
S5393 Cyclofenil Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα.
S5469 Bavachin Bavachin (Corylifolin) is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER.
S1304 Megestrol Acetate Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S8372 AZD9496 AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.
Breast Cancer Res, 2023, 25(1):96
Breast Cancer Res, 2023, 25(1):96
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
S5910 Alpha-Estradiol Alpha-Estradiol (α-Estradiol, 17 alpha-Estradiol, Alfatradiol, Epiestradiol, Epiestrol, Alora, 17 α-E2), a natural, non-feminizing stereoisomer, a hormonally almost inactive isomer of physiological 17 beta-estradiol (17 β-E2), is a weak inhibitor of estrogen.
Biomater Res, 2024, 28:0010
E2401 SPP-86 SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
S9207 Gypenoside XVII Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.GP-17 treatment predominantly up-regulating the expression of ERα but not ERβ.
S5364 DY131 DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).
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.
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.
Cancer Lett, 2024, 593:216968
Cell Death Dis, 2024, 15(8):590
Cell Death Dis, 2024, 15(7):480
S2606 Mifepristone Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Neuron, 2024, S0896-6273(24)00089-8
Cell Death Dis, 2024, 15(1):70
Cell Death Dis, 2024, 15(1):73
S7839 Endoxifen HCl Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Viruses, 2024, 16(8)1332
Blood Cancer J, 2022, 12(3):36
J Mol Cell Biol, 2021, mjab018
S6651 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.
iScience, 2024, 27(3):109125
Nutrients, 2023, 16(1)38
Chem Biol Interact, 2023, 10.1016/j.cbi.2023.110728
S8686 PHTPP PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.
J Cancer, 2022, 13(5):1573-1587
Brain Res, 2021, 1768:147580
Ecotoxicol Environ Saf, 2020, 208:111429
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.
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
Nat Genet, 2019, 51(2):207-216
S2466 Estriol Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Mol Cell, 2019, 75(6):1103-1116.e9
E1301New Imlunestrant Imlunestrant(LY3484356) is a potent, orally bioavailable selective estrogen receptor degrader (SERD) that functions as a pure antagonist of estrogen receptor alpha (ERα). It inhibits ER-dependent gene transcription and cell proliferation, resulting in sustained suppression of estrogen-driven growth in ER-positive cells.
E0361 Enclomiphene Citrate

Enclomiphene citrate is the trans isomer of clomiphene citrate and acts as a non-steroidal estrogen receptor antagonist.
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.
Biomater Res, 2024, 28:0010
S8687New MPP dihydrochloride Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein's interaction with ERα.
S8958 Camizestrant (AZD9833) Camizestrant (AZD9833) is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.
Viruses, 2024, 16(8)1332
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.
S0851 G-1 (LNS 8801) 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.
iScience, 2024, 27(3):109125
E1842New Palazestrant Palazestrant(OP-1250) is an orally bioavailable complete antagonist of estrogen receptor (ER) that blocks ER activity. It exhibits antiproliferative and antitumor activity in ER-positive (ER+) breast cancer models.
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.
iScience, 2024, 27(3):109125
Eur J Immunol, 2024, e2451226.
Pharmaceuticals (Basel), 2024, 17(3)388
S2567 MPA (Medroxyprogesterone acetate) MPA (Medroxyprogesterone acetate) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.
J Transl Med, 2024, 22(1):478
Hepatol Commun, 2024, 8(5)e0437
Cancer Rep (Hoboken), 2024, 7(1):e1934
S4154 Cholesterol Cholesterol(Cholesterin) is the principal sterol of all higher animals required to build and maintain membranes.
Clin Transl Med, 2023, 13(9):e1415
Clin Transl Med, 2023, 13(9):e1415
Biol Proced Online, 2023, 25(1):31
S1705 Progesterone Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.
Nat Commun, 2024, 15(1):8708
Dev Cell, 2024, S1534-5807(24)00326-5
Mol Med, 2024, 30(1):123
S1859 Diethylstilbestrol Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.
Biomater Res, 2024, 28:0010
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7828 Licochalcone A Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.
Br J Pharmacol, 2023, 180(8):1114-1131
Eur J Pharmacol, 2023, 957:176031
Front Oncol, 2022, 12:1006131
S1727 Levonorgestrel Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation.
Pharmaceuticals -Basel, 2022, 15-101226
J Control Release, 2021, S0168-3659(21)00550-2
Nat Cancer, 2020, 1(2):235-248
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.
Neural Plast, 2023, 2023:5225952
Front Pharmacol, 2022, 13:841941
Nutr Metab (Lond), 2021, 18(1):63
S1625 Ethinyl Estradiol Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
Hum Mol Genet, 2020, ddaa244
Regul Toxicol Pharmacol, 2020, S0273-2300(20)30246-4
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.
Chin Med, 2024, 19(1):12
Mol Med Rep, 2021, 24(4)686
Mol Med Rep, 2021, 24(4)686
S4673 Etonogestrel Etonogestrel (Implanon, Nexplanon, 3-Oxodesogestrel, 3-keto-Desogestrel) is a synthetic form of the naturally occurring female sex hormone progesterone. It binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression.
Pharmaceutics, 2024, 16(8)1030
Biomaterials, 2023, 301:122260
Breast Cancer Res, 2023, 25(1):75
S1598New Erteberel (LY500307) LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.
University of North Texas, 2014, Health Science Center at Fort Worth
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.
ACS Chem Biol, 2015, 10.1021/cb5009487
S3149 Estradiol valerate Estradiol(E2V) is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.
Front Immunol, 2022, 13:1026214
S4046 Estradiol Cypionate Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.
Nat Commun, 2024, 15(1):4549
Cell Death Dis, 2024, 15(8):590
Cell Commun Signal, 2024, 22(1):195
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.
Front Oncol, 2022, 12:857590
S3449 GSK5182 GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.
Nat Genet, 2023, 55(2):187-197
S2473 Hexestrol Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.
S2125 Mestranol Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.
S3167 Altrenogest Altrenogest (A35957, RU2267,R2267) is a progestogen structurally related to veterinary steroid trenbolone.
S5872 Estradiol dipropionate Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a semisynthetic, steroidal estrogen which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders.
Pharmaceuticals (Basel), 2022, 16(1)25
S3617 (20S)-Protopanaxatriol (20S)-Protopanaxatriol (g-PPT, 20(S)-APPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta and could modulate endothelial cell functions through the glucocorticoid receptor (GR) and estrogen receptor (ER).
S6601 (±)-Equol (±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein.
S5676 Zearalenone Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER).
E1903New SLU-PP-332 SLU-PP-332 is an agonist of pan-Estrogen Receptor/ERR with EC50 values of 98nM, 230nM, and 430 nM for ERRα, ERRβ, and ERRγ, respectively with the highest potency for ERRα. SLUPP-332 amplifies mitochondrial function and cellular respiration in skeletal muscle cell lines and also offers opportunities for researching metabolic ailments and enhancing muscle functionality.
S5288 Estropipate Estropipate (Piperazine estrone sulfate, Estrone sulfate piperazine salt, Pipestrone) is a natural estrogenic substance composed of estrone sulfate and piperazine and is used mainly in menopausal hormone therapy in the treatment of menopausal symptoms.
E0940 Propyl pyrazole triol (PPT) Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist.
S4638 Desogestrel Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.
S0358 GSK4716 GSK4716 is a selective agonist of Estrogen-Related Orphan Nuclear Receptors ERR and ERRγ with an IC50 of 2 µM in the ERRγ FRET assay.
S3657 Promestriene Promestriene (3-propyl ethyl, 17B-methyl estradiol) is a synthetic estrogen analog that has been reported to significantly improve the symptoms of vaginal atrophy caused by estrogen deprivation in topical application.
S1858 Dienestrol Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist.
Biomater Res, 2024, 28:0010
S4883 Lynestrenol Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity.
E0707 Nomegestrol Acetate Nomegestrol Acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.
S3635 Medroxyprogesterone Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist.
S4674 Hydroxyprogesterone caproate Hydroxyprogesterone Caproate (17α-Hydroxyprogesterone hexanoate, 17α-Hydroxyprogesterone caproate) is a synthetic progestational agent. It binds to and activates nuclear progesterone receptors in the reproductive system and inhibits ovulation and an alteration in the cervical mucus and endometrium.
Nat Commun, 2024, 15(1):8708
S0143 WAY-200070 WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM.
S3671 Quinestrol Quinestrol (Ethinylestradiol 3-cyclopentyl ether, EE2CPE, W-3566) is a synthetic, steroidal estrogen which is used in hormone replacement therapy and occasionally to treat breast cancer and prostate cancer.
S4097 Dydrogesterone Dydrogesterone (NSC 92336) is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus.
S0407 XCT790 XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis.
S4507 17-Hydroxyprogesterone 17-Hydroxyprogesterone (17-OHP) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
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.
S3160 Ethynodiol diacetate Ethynodiol diacetate (8080 CB,Ethynodiol acetate) is one of the first synthetic progestogens used in contraceptive pills.
S2611 Ethisterone Ethisterone(17α-Ethynyltestosterone) is a progestogen hormone being considered to treat prostate cancer.
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.
S5469 Bavachin Bavachin (Corylifolin) is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER.
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.
Nat Commun, 2024, 15(1):2377
Breast Cancer Res, 2024, 26(1):33
Toxics, 2024, 12(4)247
S7827 4-Hydroxytamoxifen (Afimoxifene) 4-Hydroxytamoxifen (Afimoxifene) is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.
Nat Commun, 2024, 15(1):2983
Cell Rep Med, 2024, 5(3):101468
Cell Rep, 2024, S2211-1247(23)01591-7
S1972 Tamoxifen Citrate Tamoxifen 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.
bioRxiv, 2024, 2023.05.10.540211
RNA, 2023, 29(9):1325-1338.
RNA, 2023, rna.079509.122
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.
Cell Death Dis, 2024, 15(4):255
Int J Mol Sci, 2023, 24(4)3356
Cells, 2022, 11(3)381
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.
Viruses, 2024, 16(8)1332
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2561 Clomifene citrate Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
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.
Viruses, 2024, 16(4)640
Endocrinology, 2021, 162(10)bqab142
bioRxiv, 2020, 2020/9/20.4.7.30734
S2167 Bazedoxifene acetate Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM).
Viruses, 2024, 16(8)1332
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Transl Oncol, 2021, 14(11):101192
S3081 Ulipristal Acetate (CDB 2914) Ulipristal acetate (CDB-2914, HRP 2000, RU 44675) is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.
J Clin Endocrinol Metab, 2019, 104(12):6256-6264
Cell Prolif, 2017, 50(5)
S1914 Pregnenolone Pregnenolone(3β-Hydroxy-5-pregnen-20-one) is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.
Cells, 2024, 13(19)1622
Biol Proced Online, 2023, 25(1):31
J Sep Sci, 2019, 42(10):1833-1841
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.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Drug Test Anal, 2020, 10.1002/dta.2917
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.
Mol Cancer Res, 2021, 19(6):1026-1039
S2301 Genistin (Genistoside) Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway.
Acta Biomater, 2021, S1742-7061(21)00586-9
S8956 (Z)-4-Hydroxytamoxifen (Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor.
iScience, 2024, 27(3):109125
Toxicol Sci, 2023, kfad049
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.
S6927 Dihydroresveratrol Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator.
E4845New Ulipristal Ulipristal(Deacetyl CDB-2914, CDB-3236) is a selective modulator of progesterone receptors used in a single dose as an emergency postcoital contraceptive.
S4629 Chlorotrianisene Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.
S5738 Megestrol Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.
S2314 Kaempferol Kaempferol, a natural flavonol, functions as an ERRα and ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation and may also inhibit the activity of fatty acid synthase.
Int J Mol Sci, 2023, 24(19)14519
Front Pharmacol, 2023, 14:1047184
Front Pharmacol, 2023, 14:1047184
S9122 Tectorigenin Tectorigenin (TEC) is an isoflavone isolated from various medicinal plants, such as Pueraria thunbergiana Benth, Belamcanda chinensis, and Iris unguicularis. It has been reported to exert pharmacological actions, including antitumor and antibacterial effects, free radical neutralization, and selective estrogen receptor modulation.
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.
S4285 Ospemifene Ospemifene(FC-1271a) is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.
S5393 Cyclofenil Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα.
S1598New Erteberel (LY500307) LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.
University of North Texas, 2014, Health Science Center at Fort Worth
E1301New Imlunestrant Imlunestrant(LY3484356) is a potent, orally bioavailable selective estrogen receptor degrader (SERD) that functions as a pure antagonist of estrogen receptor alpha (ERα). It inhibits ER-dependent gene transcription and cell proliferation, resulting in sustained suppression of estrogen-driven growth in ER-positive cells.
E4845New Ulipristal Ulipristal(Deacetyl CDB-2914, CDB-3236) is a selective modulator of progesterone receptors used in a single dose as an emergency postcoital contraceptive.
E1903New SLU-PP-332 SLU-PP-332 is an agonist of pan-Estrogen Receptor/ERR with EC50 values of 98nM, 230nM, and 430 nM for ERRα, ERRβ, and ERRγ, respectively with the highest potency for ERRα. SLUPP-332 amplifies mitochondrial function and cellular respiration in skeletal muscle cell lines and also offers opportunities for researching metabolic ailments and enhancing muscle functionality.
S8687New MPP dihydrochloride Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein's interaction with ERα.
E1842New Palazestrant Palazestrant(OP-1250) is an orally bioavailable complete antagonist of estrogen receptor (ER) that blocks ER activity. It exhibits antiproliferative and antitumor activity in ER-positive (ER+) breast cancer models.
E4947New Estrone sulfate sodium Estrone sulfate (Estrone 3-sulfate sodium salt, Premarin), an inactive form of estrogen, serves as a major circulating estrogen in the plasma. It is converted into the active form, estrone (E1), through the action of steroid sulfatase (STS. Estrone sulfate is commonly used in breast cancer research.

Choose Selective Estrogen/progestogen Receptor Inhibitors