Estrogen/progestogen Receptor

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S8372New

AZD9496

AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.

S4507New

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.

S7827New

4-Hydroxytamoxifen

4-Hydroxytamoxifen 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.

S4046

Estradiol Cypionate

Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.

S4629New

Chlorotrianisene

Chlorotrianisene is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.

S1776

Toremifene Citrate

Toremifene Citrate is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.

S2128

Bazedoxifene HCl

Bazedoxifene HCl 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.

S2561

Clomifene citrate

Clomifene Citrate is a selective estrogen receptor modulator, used in the treatment of ovulation induction.

S3081

Ulipristal

Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.

S1914

Pregnenolone

Pregnenolone is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.

S2167

Bazedoxifene Acetate

Bazedoxifene Acetate is a third generation selective estrogen receptor modulator (SERM).

S4285

Ospemifene

Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.

S1251

Dienogest

Dienogest is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.

S1376

Gestodene

Gestodene is a progestogen hormonal contraceptive.

S1377

Drospirenone

Drospirenone is a synthetic progestin that is an analog to spironolactone.

S1665

Estrone

Estrone is an estrogenic hormone.

S1709

Estradiol

Estradiol, or more precisely, 17β-estradiol, is a human sex hormone and steroid, and the primary female sex hormone.

S4673New

Etonogestrel

Etonogestrel 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.

S4674New

Hydroxyprogesterone caproate

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.

S4638New

Desogestrel

Desogestrel is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.

S4593New

Chlormadinone acetate

Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.

S2604

Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

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.

S1727

Levonorgestrel

Levonorgestrel is a female hormone that prevents ovulation.

S2567

Medroxyprogesterone acetate

Medroxyprogesterone acetate (MPA) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.

S2473

Hexestrol

Hexestrol binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.

S1705

Progesterone

Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species.

S1859

Diethylstilbestrol

Diethylstilbestrol is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.

S1625

Ethinyl Estradiol

Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.

S3149

Estradiol valerate

Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.

S2125

Mestranol

Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.

S4110

Estradiol Benzoate

Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM.

S3167

Altrenogest

Altrenogest is a progestogen structurally related to veterinary steroid trenbolone.

S7828

Licochalcone A

Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.

S3160

Ethynodiol diacetate

Ethynodiol diacetate is one of the first synthetic progestogens used in contraceptive pills.

S2611

Ethisterone

Ethisterone is a progestogen hormone being considered to treat prostate cancer.

S1191

Fulvestrant

Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay.

S1972

Tamoxifen Citrate

Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding.

S1227

Raloxifene HCl

Raloxifene is an estrogen antagonist, which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.

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.

S2832

Epiandrosterone

Epiandrosterone is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.

S2466

Estriol

Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.

S1238

Tamoxifen

Tamoxifen is an antagonist of the estrogen receptor in breast tissue.

S7839

Endoxifen HCl

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

Catalog No. Information Product Use Citations Product Validations
S8372New

AZD9496

AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.

S4507New

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.

S7827New

4-Hydroxytamoxifen

4-Hydroxytamoxifen 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.

S4046

Estradiol Cypionate

Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.

Catalog No. 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.

2015, 6(4):2315-30

2014, 13(1):230-8

2011, 6(7):e21112

S1972

Tamoxifen Citrate

Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding.

2014, Timothy E. Richardson

S1227

Raloxifene HCl

Raloxifene is an estrogen antagonist, which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.

2015, 32(6):577

2014, Health Science Center at Fort Worth

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.

2014, 24(5):528-40

2014, 9(8):e105528

S2832

Epiandrosterone

Epiandrosterone is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.

S2466

Estriol

Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.

S1238

Tamoxifen

Tamoxifen is an antagonist of the estrogen receptor in breast tissue.

2015, 6(4):2315-30

2014, Timothy E. Richardson

S7839

Endoxifen HCl

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

Catalog No. Information Product Use Citations Product Validations
S1709

Estradiol

Estradiol, or more precisely, 17β-estradiol, is a human sex hormone and steroid, and the primary female sex hormone.

S4673New

Etonogestrel

Etonogestrel 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.

S4674New

Hydroxyprogesterone caproate

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.

S4638New

Desogestrel

Desogestrel is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.

S4593New

Chlormadinone acetate

Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.

S2604

Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

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.

2015, 10.1021/cb5009487

S1727

Levonorgestrel

Levonorgestrel is a female hormone that prevents ovulation.

S2567

Medroxyprogesterone acetate

Medroxyprogesterone acetate (MPA) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.

S2473

Hexestrol

Hexestrol binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.

S1705

Progesterone

Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species.

S1859

Diethylstilbestrol

Diethylstilbestrol is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.

S1625

Ethinyl Estradiol

Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.

S3149

Estradiol valerate

Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.

S2125

Mestranol

Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.

S4110

Estradiol Benzoate

Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM.

S3167

Altrenogest

Altrenogest is a progestogen structurally related to veterinary steroid trenbolone.

S7828

Licochalcone A

Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.

S3160

Ethynodiol diacetate

Ethynodiol diacetate is one of the first synthetic progestogens used in contraceptive pills.

S2611

Ethisterone

Ethisterone is a progestogen hormone being considered to treat prostate cancer.

Catalog No. Information Product Use Citations Product Validations
S4629New

Chlorotrianisene

Chlorotrianisene is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.

S1776

Toremifene Citrate

Toremifene Citrate is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.

S2128

Bazedoxifene HCl

Bazedoxifene HCl 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.

2014, 57(3):632-41

2014, 57(3):632-41

S2561

Clomifene citrate

Clomifene Citrate is a selective estrogen receptor modulator, used in the treatment of ovulation induction.

S3081

Ulipristal

Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.

S1914

Pregnenolone

Pregnenolone is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.

S2167

Bazedoxifene Acetate

Bazedoxifene Acetate is a third generation selective estrogen receptor modulator (SERM).

S4285

Ospemifene

Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.

Catalog No. Information Product Use Citations Product Validations
S1251

Dienogest

Dienogest is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.

S1376

Gestodene

Gestodene is a progestogen hormonal contraceptive.

S1377

Drospirenone

Drospirenone is a synthetic progestin that is an analog to spironolactone.

S1665

Estrone

Estrone is an estrogenic hormone.