Enclomiphene citrate, formerly known as ICI-46476, RMI-16289 and trans-Clomiphene, is an orally bioavailable non-steroidal estrogen receptor antagonist in development for secondary hypogonadism in overweight men wishing to restore normal testicular function.
DY131 (also known as GSK-9089) is a novel selective agonist at estrogen-related receptors ERRβ and ERRγ with minimal activity at ERRα, ERα and ERβ at concentrations up to 30 μM.
Brilanestrant (formerly known as GDC-0810, ARN-810 and/or RG6046) is a novel, potent and orally bioavailable Selective Estrogen Receptor Degrader (SERD) that demonstrates robust activity in models of tamoxifen-sensitive and tamoxifen-resistant breast cancer, and is currently in clinical trials in women with locally advanced or metastatic estrogen receptor-positive breast cancer.
WAY-200070 (WAY200070) is a novel and selective agonist of the estrogen receptor β (ERRβ) with antidepressant effects.
Endoxifen E-isomer is a tamoxifen metabolite and potent SERM (Selective Estrogen Response Modifier).
GDC-0927 (formerly known as SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective ER (estrogen receptor) antagonist/ER degrader (SERD) that induces tumor regression in ER+ BC patient-derived xenograft models.
Chrysin is a novel and potent flavone.
AZD9496 (AZD-9496) maleate is a novel, potent, orally bioavailable, and selective estrogen receptor (ERα) downregulator and antagonist with anticancer activity.
GDC-0927 Racemate, the racemic mixture of GDC-0927, is used in the research of ER-related diseases.
Endoxifen, an active metabolite of Tamoxifen, is a potent and selective estrogen receptor antagonist and has been found to be effective in patients that have failed previous hormonal therapies. Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. […]