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PROTAC ERRα ligand 2 is an inverse agonist for the estrogen-related receptor α (ERRα) with an IC50 of 5.67 nM.

ERRα antagonist-1 (ERR+/- antagonist-1) is a high-affinity, selective antagonist of the estrogen-related receptor α (ERRα). It effectively prevents the interaction of ERRα with both Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, displaying IC50 values of 170 nM and 180 nM, respectively. Notably, ERRα antagonist-1 does not interfere with the interactions involving ERRβ or ERRγ and the PGC-1α and PGC-1β coactivators. Furthermore, it does not affect the interaction between either ERα or ERβ and PGC-1α or SRC-1.

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.

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.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-selective prodrug of 17β-estradiol, which has neuroprotective effects, improves cognitive dysfunction, and can be used to study brain damage.

Acolbifene (SCH 57068) is a selective antagonist of estrogen receptors with IC50s of 2 nM and 0.4 nM for estradiol-induced transcriptional activity of ERα and ERβ. Acolbifene shows an anticarcinogenic property.

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.

Estradiol 3-sulfamate (BLE 00084) is an orally active and highly potent steroidal estrone sulfatase (ES) inhibitor.Estradiol 3-sulfamate has a K(i) value of 73 nM for ES in human placental microsomes and can be used in the study of breast cancer.

Giredestrant tartrate (Estrogen receptor antagonist 1) is a novel, orally active, selective and effective non-steroidal estrogen receptor antagonist. Giredestrant tartrate strongly binds to ER, resulting in the failure of ER to activate the transcription of targeted genes and promoting the degradation of ER protein. Giredestrant tartrate can be used to treat tumor diseases.

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].

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

Pipendoxifene hydrochloride is a selective modulator of estrogen receptor.

(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.

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.

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.

CHF-4227 is a novel, potent and selective estrogen receptor modulator that reduces cholesterol and LDL cholesterol concentrations.

Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research.

Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.

Ethisterone (17α-Ethynyltestosterone) is a progestogen hormone.

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.

Cholesterol is the primary sterol in mammals, accounting for approximately 20–25% of the plasma membrane structure. It plays a key role in regulating membrane fluidity, permeability, and protein function. As an endogenous agonist of estrogen-related receptor α (ERRα), cholesterol is widely involved in metabolic regulation and serves as a precursor for the synthesis of hormones and bile acids. It is commonly used in experimental models of hyperlipidemia.

Tamoxifen Citrate is an orally active selective estrogen receptor modulator (SERM) that blocks estrogen activity in breast cells while activating estrogen signaling in cells such as those of the bone, liver, and uterus. As an Hsp90 activator, it enhances the ATPase activity of the Hsp90 chaperone complex, induces autophagy and apoptosis, and can be used to generate gene knockout models in CreER(T2) transgenic mice as well as liver injury models.

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).