Estrogen Receptors

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  1. Clomifene inhibits estrogen receptors in hypothalamus, inhibiting negative feedback of estrogen on gonadotropin release, leading to up-regulation of the hypothalamic-Cpituitary-Cadrenal axis.
  2. Dienogest is an oral progestin that has antiandrogenic activity and as a result can improve androgenic symptoms.
  3. Drospirenone is a synthetic hormone used in birth control pills.
  4. Raloxifene is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women.
  5. Aromatase inhibitor

    Fulvestrant is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.
  6. GPR119 agonist

    GSK-1292263 is a novel GPR119 agonist.
  7. Estrogen/progestogen Receptor agonist

    Hexestrol is a carcinogenic synthetic estrogen that inhibits microtubule polymerization and the formation of ribbon structures. It is an inhibitor of lipid peroxidation.
  8. ERRα and ERRγ inverse agonist

    Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.
  9. ERβ agonist

    LY500307 is a potent, selective estrogen receptor beta agonist with an EC50 of 0.66 nM.
  10. Mifepristone, an antioxidant and glucocorticoid receptor antagonist, demonstrates the ability to suppress activation of NFκB, a nuclear transcription factor that affects the expression of various adhesion molecules and several inflammatory genes.
  11. Estrogen receptor antagonist

    Tamoxifen Citrateis a selective and potent inhibitor of mammalian sterol isomerase.
  12. estrogen-receptor modulator

    Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 ?M and 2.6 ?M, respectively.
  13. Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene acetate significantly prevents bone mass loss at 20 mg/day in healthy postmenopausal women with normal or low bone mineral density.
  14. Ethisterone is a progestogen hormone.
  15. estrogen agonist

    Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
  16. Liquiritigenin is a plant-derived highly selective estrogen receptor ?? agonist
  17. Estrogen receptor degrader

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

    Tetrahydrofluoroene 52 is a potent and selective estrogen receptor β agonist.
  19. Estrogen receptor antagonist

    (E/Z)-4-hydroxy Tamoxifen 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.
  20. Estrogen receptor antagonist

    Endoxifen is a secondary metabolite of tamoxifen. It is a primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.
  21. estrogen receptor modulator

    acolbifene is a substance being studied in the prevention of breast cancer in women at high risk of breast cancer. Acolbifene hydrochloride binds to estrogen receptors in the body and blocks the effects of estrogen in the breast. It is a type of selective estrogen receptor modulator (SERM).
  22. Arzoxifene HCl is the hydrochloride salt of arzoxifene, a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist.
  23. ERRα antagonist/inverse agonist

    XCT 790 is a potent and specific inverse agonist of ERRα.
  24. ETBR antagonist

    IRL-2500 is a potent, selective ETBR antagonist. It shows some selectivity for ETB receptors (IC50 values are 1.3 and 94 nM for ETB and ETA receptors respectively).
  25. Zearalenone is a phytoestrogenic mycotoxin usually produced by Fusarium species, is shown to be a cytotoxic compound, but alos binds to the estrogen receptor (ER) (IC50 values are 166 and 240 nM for ERβ and ERα respectively) and was found to stimulate the transcriptional activity of both subtypes at concentrations between 1 - 10 nM.
  26. estrogen receptor modulator

    Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM).
  27. Estrogen modulator

    Bazedoxifene is a third generation selective modulator of estrogen receptor.
  28. ERRβ and ERRγ agonist

    DY131(GSK 9089) is a novel selective agonist of ERRα and ERRβ.
  29. Estrogen receptor modulator

    Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis.
  30. estrogen receptor downregulator and antagonist

    AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator and antagonist.
  31. Estrogen receptor degrader

    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.
  32. SERD/SERM

    RAD1901 is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities.
  33. Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
  34. Chlorotrianisene is a synthetic, non-steroidal estrogen.
  35. selective estrogen receptor modulator (SERM)

    Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.
  36. ERRβ & ERRγ Agonist

    GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ
  37. Estrogen receptor agonist

    (R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
  38. ER antagonist

    Fulvestrant S enantiomer is the S enantiomer of Fulvestrant. Fulvestrant is a selective estrogen receptor (ER) antagonist which can be used to treat breast cancer.
  39. ERβ receptor antagonist

    PHTPP is a pyrazolo[1,5-α]pyrimidine-based ligand that acts as a full antagonist of estrogen ERβ receptors with 36-fold selectivity over ERα.
  40. Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
  41. selective Estrogen receptor modulator

    Lasofoxifene tartrate is a third-generation selective estrogen receptor modulator.
  42. PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
  43. EStrogen receptor (ER) antagonist

    GW7604 is an antiestrogen agbent, and is tthe presumed metabolite of GW5638 in breast (MCF-7) and endometrial (ECC-1) cell lines in vitro.
  44. ERRα Degrader

    PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader.
  45. ERRα inverse agonist

    PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).
  46. ERRγ agonist

    GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.
  47. estrogen receptor degrader

    LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM.
  48. estrogen ligand

    Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.
  49. estrogen receptor antagonist

    GDC-0927 (SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist.
  50. estrogen receptor covalent antagonist

    H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively.

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