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

Ligand: WAY200070 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pEC50
Reference (Journal): WAY-200070, a selective agonist of estrogen receptor beta as a potential novel anxiolytic/antidepressant agent.
Published in: Neuropharmacology

Ligand: WAY200070 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.
Published in: J Med Chem

Ligand: tamoxifen (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity: 7.16 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)
Median affinity: 7.17 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: R,R-THC (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.4399995803833 pKi
Reference (Journal): Novel ligands that function as selective estrogens or antiestrogens for estrogen receptor-alpha or estrogen receptor-beta.
Published in: Endocrinology

Ligand: R,R-THC (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.4399995803833 pKi
Reference (Journal): Estrogen receptor subtype-selective ligands: asymmetric synthesis and biological evaluation of cis- and trans-5,11-dialkyl- 5,6,11, 12-tetrahydrochrysenes.
Published in: J Med Chem

Ligand: raloxifene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997), EMA (1998)
Primary target: yes
Median affinity: 8 pKi
Reference (Journal): 2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.
Published in: Bioorg Med Chem Lett

Ligand: prinaberel (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.430000305175781 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: 8.510000228881836 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: 8.300000190734863 pIC50
Reference (Journal): Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.
Published in: J Med Chem

Ligand: prinaberel (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Selective estrogen receptor-beta agonists repress transcription of proinflammatory genes.
Published in: J Immunol

Ligand: PHTPP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.900000095367432 pKi
Reference (Journal): Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains.
Published in: J Med Chem

Ligand: ospemifene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2013), EMA (2015)
Primary target: yes
Median affinity: 6.389999866485596 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: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.559999942779541 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: lasofoxifene (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 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: (S)-liquiritigenin (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.440000057220459 pEC50
Reference (Journal): Liquiritigenin is a plant-derived highly selective estrogen receptor beta agonist.
Published in: Mol Cell Endocrinol

Ligand: HPTE (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.64 pKi
Reference (Journal): Signalling by CXC-chemokine receptors 1 and 2 expressed in CHO cells: a comparison of calcium mobilization, inhibition of adenylyl cyclase and stimulation of GTPgammaS binding induced by IL-8 and GROalpha.
Published in: Br J Pharmacol

Ligand: genistein (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: fulvestrant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2004)
Primary target: yes
Median affinity: 8.859999656677246 pKi
Reference (Journal): De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor.
Published in: J Med Chem

Ligand: FERb 033 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.319999694824219 pEC50
Reference (Journal): Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta.
Published in: J Med Chem

Ligand: FERb 033 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.149999618530273 pKi
Reference (Journal): Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta.
Published in: J Med Chem

Ligand: ethinylestradiol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 8.09000015258789 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
Median affinity: 7.93 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
Median affinity: 8.4 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: diethylstilbestrol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1973)
Median affinity: 9.8 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology

Ligand: diarylpropionitrile (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.069999694824219 pEC50
Reference (Journal): Estrogen receptor alpha and beta specific agonists regulate expression of synaptic proteins in rat hippocampus.
Published in: Brain Res

Ligand: diarylpropionitrile (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists.
Published in: J Med Chem

Ligand: diarylpropionitrile (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
Published in: J Med Chem

Ligand: bisphenol A (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5.960000038146973 pEC50
Reference (Journal): Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERα-selective antagonist.
Published in: Bioorg Med Chem Lett

Ligand: bazedoxifene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2009), FDA (2013)
Primary target: yes
Median affinity: 7.070000171661377 pIC50
Reference (Journal): Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.
Published in: J Med Chem

Ligand: AC-186 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.220000267028809 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
Median affinity: 10.6 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)
Median affinity: 9.34 pKi
Reference (Journal): Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
Published in: Endocrinology