- Hydroxyprogesterone caproate is a synthetic, steroidal progestin; an ester derivative of 17?α-hydroxyprogesterone formed from caproic acid.
- Protirelin is a thyrotropin-releasing hormone receptor used to treat hypothyroidism.
- Desogestrel is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.
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GPR139 antagonist
NCRW0005-F05, first antagonist selective for GPR139 (IC50 value 0.21 uM); a useful tool to study GPR139 pharmacology, especially in combination with the GPR139 agonist JNJ 63533054. -
RORγ modulator
RORγ modulator 1 is a retinoid-related orphan receptor gamma (RORy) modulator, extracted from patent WO/2015061515 A1, example 124. - Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
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GPR39 agonist
TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).- Urszula Doboszewska, .et al. , Cell Mol Life Sci, 2023, Apr 25;80(5):133 PMID: 37185787
- Urszula Doboszewska, .et al. , Cells, 2023, Jan 9;12(2):264 PMID: 36672199
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angiotensin II receptor type 1 antagonist
Azilsartan medoxomil is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. - Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive.
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glucocorticoid receptor agonist
Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. -
GPR35/CXCR8 agonist
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8. - Vitamin D2 (Ergocalciferol) is a form of vitamin D, used as a vitamin D supplement.
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GPR55 antagonist
CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. -
RORγ agonist
LYC-55716 is novel oral RAR-related orphan receptor γ (RORγ) agonist. -
Aldosterone Receptor Antagonist
Esaxerenone, also known as CS-3150, XL-550, is a nonsteroidal antimineralocorticoid that acts as a highly selective silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over other steroid hormone receptors, and 4-fold and 76-fold higher affinity for the MR relative to the existing antimineralocorticoids spironolactone and eplerenone. -
RORγt inhibitor
AGN-242428, also known as VTP-43742, is a potent, selective and orally active RORγt inhibitor for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis. -
ERRβ & ERRγ Agonist
GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
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synthetic glucocorticoid receptor agonist
Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent. -
Estrogen receptor agonist
(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.- Gao X, .et al. , Toxins (Basel), 2020, Jan 26;12(2) PMID: 31991913
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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. -
FAA1 agonist
FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54. - Androsterone is a steroid hormone produced in the body from 5α-reduced metabolites of dehydroepiandrosterone. It is the major androgen excreted in urine as a metabolite of testosterone and is used as the international reference standard for androgenic activity.
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glucocorticoid receptor agonist
Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone. -
Estrogen receptor ligand
α-Estradiol is an endogenous estrogen receptor ligand (Ki values are 0.2 and 1.2 nM for ERα and ERβ receptors respectively). -
glucocorticoid agonist
Beclometasone dipropionate is a potent glucocorticoid agonist; it is a prodrug of the free form, beclometasone. - Medroxyprogesterone is used in the treatment of renal carcinoma. It is a synthetic progestational hormone used in veterinary practice as an estrus regulator.
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Androgen receptor antagonist
Spironolactone is a potent antagonist of the androgen receptor. -
non-peptide angiotensin II receptor antagonist
Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Through oral administration, fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as systemic vasoconstriction and water retention by the kidneys. - Estropipate is a form of estrogen, an estrogen receptor agonist. It has several uses such as: Alleviate symptoms of menopause as hormone replacement therapy, treatment some types of infertility, treatment of some conditions leading to underdevelopment of female sexual characteristics, and treatment of prostate cancer and prevention of osteoporosis.
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glucocorticoid
Fluorometholone is a glucocorticoid employed, usually as eye drops, in the treatment of allergic and inflammatory conditions of the eye. It has also been used topically in the treatment of various skin disorders. -
GnRH/LHRH receptor agonist
Leuprorelin is a Gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, LHRH) receptor agonist. Suppresses estradiol, LH and FSH serum levels and represses the growth of experimental rat endometriosis. -
GnRH agonist
Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH. - Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
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selective Estrogen receptor modulator
Lasofoxifene tartrate is a third-generation selective estrogen receptor modulator. -
thromboxane A2 (TXA2) receptor (TP receptor) antagonist
Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma. -
glucocorticoid receptor agonist
Beclometasone, also known as Beclomethasone, is an anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma. - Norethindrone acetate is used in combination with estrogen as a contraceptive (oral). It is reasonably anticipated to be a human carcinogen.


