Estrogen Receptor/ERR

Tamoxifen (ICI47699) is a selective and orally effective estrogen receptor modulator (SERM). Tamoxifen has both inhibitory (e.g., mammary cells) and activating (e.g., bone, liver, and uterine cells) activity against estrogens.

Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist (IC50=9.4 nM) and an agonist of GPR30. Fulvestrant has antitumor activity, inhibiting cell proliferation and inducing apoptosis and autophagy.

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

(E Z)-4-Hydroxytamoxifen (Afimoxifene) is a novel estrogen inhibitor, commonly used in research for various estrogen-dependent conditions, including cyclic mastalgia and gynecomastia.

Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.

Cholesterol (cholesteryl alcohol) is a natural product that is the major sterol in mammals and an agonist of estrogen-related receptor α (ERRα). Cholesterol is widely found in the cell membranes of animals and is also used in the synthesis of several important hormones and bile acids.

Saikosaponin D is a novel SERCA inhibitor by inhibiting NF-κB and STAT3 signaling to protect against acetaminophen-induced hepatotoxicity.

Liquiritigenin (4',7-Dihydroxyflavanone), a flavonoid aglycone from licorice, is a highly selective estrogen receptor β (ERβ) agonist.

Coumestrol that existed in soybean products suppresses the proliferation of ES2 cells (IC50: 50 μM). It exhibits activities against neurological disorders, cancers and autoimmune diseases.

Giredestrant (GDC-9545) potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity. Giredestrant, a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

Bazedoxifene acetate (WAY-TES 424) is a novel selective estrogen receptor modulator (SERM).

GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM)

G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).

Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant  is an orally available selective estrogen receptor degrader .

Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Delphinidin chloride, a natural plant pigment found in berries and red wine, is a precursor of certain anthocyanins. Delphinidin chloride induces the release of nitric oxide from the vascular endothelium, resulting in vascular relaxation. At the dose of 1-40 μM, epithelial growth factor receptor signaling and estrogen receptor α expression were inhibited, which was associated with apoptosis and autophagy. Delphinidin chloride regulates JAK STAT3 and MAPKinase signaling. Delphinidin also inhibited the histone acetyltransferase activity of p300 CBP (IC50 was about 30 μM).

Erteberel (LY500307) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.

Tracheloside significantly decreases the activity of alkaline phosphatase (IC50: 0.31 μg ml), a level of inhibition comparable to that of tamoxifen (IC50: 0.43 μg ml).

(Rac)-Acolbifene (EM-343) is the racemic form of Acolbifene. Acolbifene is a estrogen receptor antagonist. (Rac)-Acolbifene exhibits anti-estrogenic and estrogenic activities. (Rac)-Acolbifene contains a piperidine ring and exhibits good pharmacological profile,relative binding affinity (RBA)=380.

Droloxifene (3-Hydroxytamoxifen), a tamoxifen derivative, is an oral active and selective estrogen receptor modulator.Droloxifene induced p53 expression and apoptosis in McF-7 cells.Fluroxifene has anti-estrogen and anti-implantation effects.Fluroxifene prevented bone loss in ovariectomized rats.

Propyl pyrazole triol (PPT) is a selective agonist of estrogen receptor alpha (ERα), exhibiting a relative binding affinity of 49% for ERα, which is approximately 410 times higher than its affinity for estrogen receptor beta (ERβ: 0.12%).

1. Isocurcumenol inhibits 5α-reductase which converts testosterone to dihydrotestosterone (DHT).

Amcenestrant (SAR439859) is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 nM for ERα degradation).

Premarin (Estrone 3-sulfate) is an an estrogen sulfate with neuroprotective actions during traumatic brain injury.

G15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM)

Camizestrant TFA (AZD-9833 TFA) is a potent and orally active antagonist of estrogen receptor (ER).

α-Zearalenol is one of the major metabolites of Zearalenone. α-Zearalenol has structural analogy to estrogen, thus α-Zearalenol can bind to estrogen receptors (ERs).

kaempferide (4'-Methylkaempferol) inhibits the proliferation of native and estrogen receptor beta overexpressing colon cancer cells through a mechanism not mediated by ligand binding dependent estrogen receptor activation.

DPN (Diarylpropionitrile) is an selective agonist of estrogen receptor β (ERβ) .

XCT790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα).

Enclomiphene citrate (trans-Clomiphene citrate) is a non-steroidal estrogen receptor antagonist,with antioestrogenic property

Segetalin B is a natural product from Vaccaria segetalis (Neck.) Garcke, has estrogen-like activity.

G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.

Estradiol benzoate (Benzhormovarine) is the synthetic benzoate ester of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.

Chrysin (5,7-Dihydroxyflavone) exhibits many biological activities and pharmacological effects, including antioxidant, anti-inflammatory, anticancer, and antiviral activities.

Norethindrone acetate (19-Norethindroneacetate) is an oestrogen with inhibitory effects on adolescent menstruation and hepatic adenomas and is often used in combination with progestins in the study of endometriosis.

Genistin (Genistoside) is the major isoflavonoid of soybeans and soy products.It has been reported to possess various therapeutic effects, including anti-inflammatory and anticancer activities

Camizestrant (Estrogen receptor antagonist 2) is an antagonist of the estrogen receptor and can be used in studies about ER+ HER2-advanced breast cancer[1].

Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM).

Estriol (Oestriol) is a hydroxylated metabolite of ESTRADIOL or ESTRONE that has a hydroxyl group at C3, 16-alpha, and 17-beta position. Estriol is a major urinary estrogen. During PREGNANCY, a large amount of estriol is produced by the PLACENTA.

Nylestriol (LY 49825) is an agonist of estrogen receptor.

Etonogestrel (Implanon) is a steroidal progestin used as hormonal contraceptives.

Clomiphene citrate (NSC 35770) is a selective estrogen receptor modulator.

Prochloraz (Prelude) is a broad-spectrum contact imidazole fungicide. Prochloraz inhibits human placental microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an estrogen receptor (IC50s = 25 μM) and androgen receptor (IC50 = 4 μM) antagonist, and activates aryl hydrocarbon receptors (EC50 = 1 μM).

AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity.

H3B-5942 belongs to a class of ERα antagonists referred to as selective estrogen receptor covalent antagonists (SERCA).