Target family: 3A. Estrogen receptors (type: nhr)
Target: Estrogen receptor-&alpha;

Ligand: WAY200070 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.809999942779541 pEC50
Reference (Journal): WAY-200070, a selective agonist of estrogen receptor beta as a potential novel anxiolytic/antidepressant agent.
Published in: Neuropharmacology

Ligand: tibolone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA (2013)
Primary target: no
Median affinity: 8.399999618530273 pEC50
Reference (Journal): Regulation of activities of steroid hormone receptors by tibolone and its primary metabolites.
Published in: J Steroid Biochem Mol Biol

Ligand: tamoxifen (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: yes
Median affinity: 7.820000171661377 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: tamoxifen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: yes
Median affinity: 7.800000190734863 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: stanozolol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1962)
Primary target: no
Median affinity: 6.949999809265137 pIC50
Reference (Webpage): DrugMatrix in vitro pharmacology data

Ligand: R,R-THC (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.38 pKi
Reference (Journal): Novel ligands that function as selective estrogens or antiestrogens for estrogen receptor-alpha or estrogen receptor-beta.
Published in: Endocrinology

Ligand: raloxifene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997), EMA (1998)
Primary target: yes
Median affinity: 9.5 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: raloxifene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1997), EMA (1998)
Primary target: no
Median affinity: 9.5 pKi
Reference (Journal): Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists.
Published in: J Med Chem

Ligand: propylpyrazoletriol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.640000343322754 pKi
Reference (Journal): Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists.
Published in: J Med Chem

Ligand: propylpyrazoletriol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.640000343322754 pKi
Reference (Journal): Conformational changes and coactivator recruitment by novel ligands for estrogen receptor-alpha and estrogen receptor-beta: correlations with biological character and distinct differences among SRC coactivator family members.
Published in: Endocrinology

Ligand: prinaberel (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.210000038146973 pIC50
Reference (Journal): Selective estrogen receptor-beta agonists repress transcription of proinflammatory genes.
Published in: J Immunol

Ligand: prinaberel (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.119999885559082 pIC50
Reference (Journal): Selective estrogen receptor-beta agonists repress transcription of proinflammatory genes.
Published in: J Immunol

Ligand: prinaberel (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.920000076293945 pIC50
Reference (Journal): Selective estrogen receptor-beta agonists repress transcription of proinflammatory genes.
Published in: J Immunol

Ligand: ospemifene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2013), EMA (2015)
Primary target: yes
Median affinity: 6.420000076293945 pKi
Reference (Journal): Vaginal effects of ospemifene in the ovariectomized rat preclinical model of menopause.
Published in: J Steroid Biochem Mol Biol

Ligand: norendoxifen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.769999980926514 pEC50
Reference (Journal): Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.
Published in: J Med Chem

Ligand: methyl-piperidino-pyrazole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.57 pKi
Reference (Journal): Antagonists selective for estrogen receptor alpha.
Published in: Endocrinology

Ligand: LSZ102 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.520000457763672 pIC50
Reference (Journal): Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
Published in: J Med Chem

Ligand: lasofoxifene (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.510000228881836 pIC50
Reference (Journal): Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
Published in: J Med Chem

Ligand: imlunestrant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.510000228881836 pKi
Reference (Patent): Selective estrogen receptor degraders

Ligand: hexestrol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.3 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: GSK5182 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.489999771118164 pIC50
Reference (Journal): Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
Published in: Bioorg Med Chem Lett

Ligand: giredestrant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.300000190734863 pIC50
Reference (Journal): GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
Published in: J Med Chem

Ligand: fulvestrant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2004)
Primary target: yes
Median affinity: 8.979999542236328 pKi
Reference (Journal): De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor.
Published in: J Med Chem

Ligand: ethinylestradiol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.
Published in: J Med Chem

Ligand: estrone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: yes
Median affinity: 8.5 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: estriol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: yes
Median affinity: 8.670000076293945 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: ERD-308 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER).
Published in: J Med Chem

Ligand: diarylpropionitrile (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.179999828338623 pEC50
Reference (Journal): Estrogen receptor alpha and beta specific agonists regulate expression of synaptic proteins in rat hippocampus.
Published in: Brain Res

Ligand: compound 17b [PMID: 35286086] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.34000015258789 pIC50
Reference (Journal): Gefitinib-Tamoxifen Hybrid Ligands as Potent Agents against Triple-Negative Breast Cancer.
Published in: J Med Chem

Ligand: clomiphene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity: 8.890000343322754 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: camizestrant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pIC50
Reference (Journal): Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Published in: J Med Chem

Ligand: bazedoxifene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2009), FDA (2013)
Primary target: yes
Median affinity: 7.639999866485596 pIC50
Reference (Journal): Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.
Published in: J Med Chem

Ligand: amcenestrant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3<i>S</i>)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7<i>H</i>-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer.
Published in: J Med Chem

Ligand: AC-186 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): AC-186, a selective nonsteroidal estrogen receptor β agonist, shows gender specific neuroprotection in a Parkinson's disease rat model.
Published in: ACS Chem Neurosci

Ligand: 4-hydroxytamoxifen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
Published in: Bioorg Med Chem Lett

Ligand: 4-hydroxytamoxifen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.85 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: 4-hydroxytamoxifen (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.85 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: 17β-estradiol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1954, prior history unavailable)
Primary target: yes
Median affinity: 9.819999694824219 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: 16α-hydroxyestrone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Covalent binding of the endogenous estrogen 16 alpha-hydroxyestrone to estradiol receptor in human breast cancer cells: characterization and intranuclear localization.
Published in: Proc Natl Acad Sci U S A