ESR1
ENSG00000091831
Target class
Nuclear receptor
Chromosome
6
Approved drugs
31
Clinical candidates (approved and in development)
48
- Approved drugs
- 31
- Clinical candidates (approved and in development)
- 48
- Chemical probe available
- Yes
- Target name
- ESR1
- Gene name
- Estrogen receptor 1
- Gene symbol
- ESR1
- Previous gene symbols
- ESR
- Protein name
- Estrogen receptor (ER) (ER-alpha) (Estradiol receptor) (Nuclear receptor subfamily 3 group A member 1)
- ER
- NR3A1
- Era
- ER-alpha
- Gene biotype
- Protein coding
- Gene family
- Estrogen receptors
- Target class
- Nuclear receptor
- Target type
- Human gene
- Tissues expressed in
- 23
- Protein localisation evidence grade
- Approved
- Highest tissue expression
- 88.87
- Tissue specificity (Gini)
- 0.829
- Tissue specificity (tau)
- 0.944
- KEGG gene identifiers
- hsa:2099
- Protein interaction confidence
- 0.853932
- Protein interaction partners
- 250
- R-HSA-1251985
- R-HSA-1257604
- R-HSA-2219530
- R-HSA-383280
- R-HSA-4090294
- R-HSA-5689896
- R-HSA-6811558
- R-HSA-8866910
- R-HSA-8931987
- R-HSA-8939211
- R-HSA-8939256
- R-HSA-8939902
- R-HSA-9009391
- R-HSA-9018519
- R-HSA-9841251
- R-HSA-9927418
- R-HSA-9927426
- End position
- 152129619
- Start position
- 151651284
- Chromosome
- 6
- Strand
- Forward
- [Isoform 1]: Nucleus . Cytoplasm . Cell membrane
- Peripheral membrane protein
- Cytoplasmic side . Note=A minor fraction is associated with the inner membrane.
- SUBCELLULAR LOCATION: [Isoform 3]: Nucleus. Cytoplasm. Cell membrane
- Peripheral membrane protein
- Cytoplasmic side. Cell membrane
- Single-pass type I membrane protein. Note=Associated with the inner membrane via palmitoylation (Probable). At least a subset exists as a transmembrane protein with a N-terminal extracellular domain. .
- SUBCELLULAR LOCATION: Nucleus. Golgi apparatus. Cell membrane. Note=Colocalizes with ZDHHC7 and ZDHHC21 in the Golgi apparatus where most probably palmitoylation occurs. Associated with the plasma membrane when palmitoylated.
- Nucleoplasm
- Vesicles
- PubMed 12682286
- PubMed 20074560
- PubMed 24498420
- Tissue specificity (tau)
- 0.943702
- Expression inequality (Gini)
- 0.829309
Expression in transcripts per million
- Cervix - Endocervix
- 88.87
- Uterus
- 60.73
- Cervix - Ectocervix
- 48.65
- Vagina
- 45.57
- Fallopian Tube
- 43.24
Expression in transcripts per million
- Cervix - Endocervix88.87
- Uterus60.73
- Cervix - Ectocervix48.65
- Vagina45.57
- Fallopian Tube43.24
- Ovary7.72
- Pituitary5.82
- Breast - Mammary Tissue5.76
- Prostate5.07
- Liver3.53
- Artery - Tibial2.77
- Testis2.74
- Artery - Aorta2.72
- Thyroid2.55
- Artery - Coronary2.52
- Nerve - Tibial2.13
- Adipose - Subcutaneous2.07
- Bladder1.97
- Lung1.81
- Adipose - Visceral (Omentum)1.57
- Spleen1.35
- Brain - Cerebellum1.33
- Adrenal Gland1.07
- Brain - Cerebellar Hemisphere0.88
- Esophagus - Gastroesophageal Junction0.88
And 29 more, listed on the interactive page.
- GO:0000122
- GO:0007165
- GO:0010629
- GO:0030520
- GO:0032355
- GO:0043124
- GO:0043627
- GO:0045893
- GO:0045944
- GO:0051123
- GO:0071168
- GO:0071392
- GO:1902894
- GO:0000785
- GO:0000791
- GO:0005634
- GO:0005654
- GO:0005737
- GO:0005829
- GO:0005886
- GO:0032991
- GO:0000978
- GO:0001093
- GO:0001221
- GO:0001222
- GO:0001223
- GO:0001228
- GO:0003682
- GO:0004879
- GO:0005515
- GO:0005516
- GO:0008013
- GO:0017025
- GO:0019899
- GO:0019901
- GO:0030284
- GO:0030331
- GO:0034056
- GO:0042802
- GO:0051117
- GO:0071889
- GO:1990837
Increased, adenosquamous carcinomas of endometrium
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourceAltered, Larval development
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourceN/A, Breast Cancer
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourceimpacts sexual development
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- reproductive
PubMed 38773351vaginal atrophy
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- reproductive
PubMed 38773351Decrease, Population growth rate
Effects
- Inhibition/Decrease/Downregulation
Studies
- cell-based
Evidence sourceHot flashes
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
PubMed 38773351Decrease, Population growth rate
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourcePromotion, ovarian adenomas
Effects
- Inhibition/Decrease/Downregulation
Studies
- cell-based
Biological samples
- hypothalamus
Evidence sourcePromotion, ovarian granular cell tumors
Effects
- Inhibition/Decrease/Downregulation
Studies
- cell-based
Biological samples
- hypothalamus
Evidence sourcebreast tissue growth in males
Effects
- Activation/Increase/Upregulation
Studies
- clinical
Biological samples
- reproductive
PubMed 38773351Decreased sperm quantity / quality in the adult, Decreased fertility
Studies
- cell-based
Evidence sourcebreast atrophy
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- reproductive
PubMed 38773351irregular menstruation in females
Effects
- Activation/Increase/Upregulation
Studies
- clinical
Biological samples
- reproductive
PubMed 38773351Increase, Endometrial adenocarcinomas
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourceAltered, Reproductive behaviour
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourceIncreased risk of thrombosis
Effects
- Activation/Increase/Upregulation
Studies
- clinical
Biological samples
- CV
PubMed 38773351Impaired development of, Reproductive organs
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourceosteoporosis
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- bone
PubMed 38773351
regulation of steroid biosynthetic process
- cell-based: CEETOX_H295R_ESTRONE, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_ESTRADIOL, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_TESTO, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_ESTRADIOL, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_TESTO, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_ESTRONE, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
Biological samples
- H295R, cell line
Evidence sourceregulation of transcription factor activity
- cell-based: TOX21_ERa_BLA_Antagonist_ratio is an assay readout measuring reporter gene via receptor activity and designed using inducible reporter (beta lactamase induction) detected with GAL4 b-lactamase reporter gene. The signal is derived from the ratio of cleaved (ch2) to uncleaved (ch1) reporter gene substrate used as the measure of target activity.
- cell-based: ATG_ERa_TRANS, is one of 30 assay component(s) measured or calculated from the ATG_TRANS assay. It is designed to make measurements of mRNA induction, a form of inducible reporter, as detected with fluorescence intensity signals by Reverse transcription polymerase chain reaction (RT-PCR) and Capillary electrophoresis technology.
- cell-based: TOX21_ERa_LUC_VM7_Antagonist_Specificity, is one of one assay component(s) measured or calculated from the TOX21_ERa_LUC_VM7_Antagonist_Specificity assay. It is designed to make measurements of luciferase induction, a form of inducible reporter, as detected with bioluminescence signals by luciferase-coupled ATP quantitation technology.
- cell-based: ATG_ERE_CIS, is one of 52 assay component(s) measured or calculated from the ATG_CIS assay. It is designed to make measurements of mRNA induction, a form of inducible reporter, as detected with fluorescence intensity signals by Reverse transcription polymerase chain reaction (RT-PCR) and Capillary electrophoresis technology.
- cell-based: TOX21_ERa_BLA_Agonist_ratio is an assay readout measuring reporter gene via receptor activity and designed using inducible reporter (beta lactamase induction) detected with GAL4 b-lactamase reporter gene. The signal is derived from the ratio of cleaved (ch2) to uncleaved (ch1) substrate used as the measure of target activity.
- cell-based: TOX21_ERa_LUC_VM7_Antagonist is one of one assay component(s) measured or calculated from the TOX21_ERa_LUC_VM7_Antagonist assay. It is designed to make measurements of luciferase induction, a form of inducible reporter, as detected with bioluminescence signals by luciferase-coupled ATP quantitation technology.
- cell-based: ATG_ERa_TRANS, is one of 30 assay component(s) measured or calculated from the ATG_TRANS assay. It is designed to make measurements of mRNA induction, a form of inducible reporter, as detected with fluorescence intensity signals by Reverse transcription polymerase chain reaction (RT-PCR) and Capillary electrophoresis technology.
- cell-based: TOX21_ERa_LUC_VM7_Agonist, is one of one assay component(s) measured or calculated from the TOX21_ERa_LUC_VM7_Agonist assay. It is designed to make measurements of luciferase induction, a form of inducible reporter, as detected with bioluminescence signals by luciferase-coupled ATP quantitation technology.
- cell-based: ATG_ERE_CIS, is one of 52 assay component(s) measured or calculated from the ATG_CIS assay. It is designed to make measurements of mRNA induction, a form of inducible reporter, as detected with fluorescence intensity signals by Reverse transcription polymerase chain reaction (RT-PCR) and Capillary electrophoresis technology.
- VM7, cell line
- HEK293T, cell line
- HepG2, cell line
Evidence sourceprotein stabilization
- cell-based: OT_ER_ERaERb_1440, is one of one assay component(s) measured or calculated from the OT_ER_ERaERb_1440 assay. It is designed to make measurements of protein fragment complementation, a form of binding reporter, as detected with fluorescence intensity signals by Protein-fragment Complementation technology.
- cell-based: OT_ER_ERaERa_0480, is one of one assay component(s) measured or calculated from the OT_ER_ERaERa_0480 assay. It is designed to make measurements of protein fragment complementation, a form of binding reporter, as detected with fluorescence intensity signals by Protein-fragment Complementation technology.
- cell-based: OT_ER_ERaERb_0480, is one of one assay component(s) measured or calculated from the OT_ER_ERaERb_0480 assay. It is designed to make measurements of protein fragment complementation, a form of binding reporter, as detected with fluorescence intensity signals by Protein-fragment Complementation technology.
- cell-based: OT_ER_ERaERa_1440, is one of one assay component(s) measured or calculated from the OT_ER_ERaERa_1440 assay. It is designed to make measurements of protein fragment complementation, a form of binding reporter, as detected with fluorescence intensity signals by Protein-fragment Complementation technology.
Biological samples
- HEK293T, cell line
Evidence sourceregulation of steroid hormone biosynthetic process
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
Biological samples
- H295R, cell line
Evidence sourcereceptor binding
Studies
- biochemical: NVS_NR_hER, is one of one assay component(s) measured or calculated from the NVS_NR_hER assay. It is designed to make measurements of radioligand binding, a form of binding reporter, as detected with scintillation counting signals by Lysate-based radiodetection technology.
Biological samples
- cell-free
Evidence sourceregulation of gene expression
- cell-based: OT_ERa_GFPERaERE_0120, is one of one assay component(s) measured or calculated from the OT_ERa_GFPERaERE_0120 assay. It is designed to make measurements of fluorescent protein induction, a form of inducible reporter, as detected with optical microscopy: fluorescence microscopy signals by Microscopy technology.
- cell-based: OT_ERa_GFPERaERE_0480, is one of one assay component(s) measured or calculated from the OT_ERa_GFPERaERE_0480 assay. It is designed to make measurements of fluorescent protein induction, a form of inducible reporter, as detected with optical microscopy: fluorescence microscopy signals by Microscopy technology.
Biological samples
- HeLa, cell line
Evidence sourcecell proliferation
Studies
- cell-based: ACEA_ER_80hr, is one of two assay component(s) measured or calculated from the ACEA_ER assay. It is designed to make measurements of real-time cell-growth kinetics, a form of growth reporter, as detected with electrical impedance signals by Real-Time Cell Electrode Sensor (RT-CES) technology.
Biological samples
- T47D, cell line
Evidence source
Related records
Trials (2,456)
- "E4/DRSP Endocrine Function, Metabolic Control and Hemostasis Study"
- "Effect of Central Insulin Administration on Whole-body Insulin Sensitivity in Women"
- "Effect of CPA/EE Drug on Periodontal Tissue and hsCRP Levels in PCOS Patients With Gingivitis
- "Neo-Adjuvant Treatment With Palbociclib: Effect on Ki67 and Apoptosis Before, During and After Treatment "
- "Quick-starting" of a New Combined Hormonal Contraceptive Pills, 15 mg Estetrol/3 mg Drospirenone VS 20 mcg Ethinylestradiol/75 mcg Gestodene Focusing on Ovulation Inhibition
- "Quick-starting" of a Quadriphasic Contraceptive Pills, 1 - 3 mg Estradiol Valerate/ 2 - 3 mg Dienogest VS 20 mcg Ethinylestradiol/75 mcg Gestodene Focusing on Ovulation Inhibition
- (VELA) Study of BLU-222 in Advanced Solid Tumors
- [177Lu]Lu-NeoB in Combination With Ribociclib and Fulvestrant in Participants With ER+, HER2- and GRPR+ Advanced Breast Cancer
- 1303GCC: Trastuzmab & Pertuzumab With Hormonal Therapy or Chemotherapy in Women Aged 60 and Over.
- 2-Year Therapy With Teriparatide vs 1-yr Therapy Followed by 1-Year of Raloxifene or Calcium/Vit D in Severe Postmenopausal Osteoporosis
- 3-year Study of Menostar Versus Evista to Prevent Osteoporosis in Post-menopausal Women
- 4-Hydroxytamoxifen or Tamoxifen Citrate in Treating Women With Newly Diagnosed Ductal Breast Carcinoma in Situ
- 71A/G HSD17B5 SNP and Effects of Oral Contraceptive Pill in PCOS Women
- A Bioequivalence Study of Norgestimate /Ethinyl Estradiol (NGM/EE) Tablets Manufactured at 2 Different Facilities
- A Biomarker Study of Palbociclib + Fulvestrant for Second, and Third Line of Postmenopausal Women With hr+/her2- Advanced Breast Cancer
- A Chemoprevention Study of an Investigational Drug in Men With High Grade Prostate Intraepithelial Neoplasia (PIN)
- A Clinical Study of JS105 in Combination With Other Anti-tumor Therapies in Patients With Solid Tumors
- A Clinical Study to Assess the Safety of a New Influenza Vaccine
- A Clinical Study to Evaluate Ospemifene in the Treatment of Vulvar and Vaginal Atrophy in Postmenopausal Women
- A Clinical Study to Evaluate the Efficacy and Safety of Ospemifene in the Treatment of Vulvar and Vaginal Atrophy (VVA) in Postmenopausal Women
Drugs (55)
- Acolbifene Estrogen receptor modulator
- Afimoxifene Estrogen receptor modulator
- Allylestrenol Estrogen receptor agonist
- Amcenestrant Estrogen receptor alpha degrader
- Arzoxifene Estrogen receptor modulator
- Bazedoxifene Estrogen receptor modulator
- Bazedoxifene acetate Estrogen receptor modulator
- Brilanestrant Estrogen receptor degrader
- Camizestrant Estrogen receptor alpha degrader
- CHF4227 Estrogen receptor modulator
- Clomiphene Estrogen receptor alpha modulator
- Clomiphene citrate Estrogen receptor alpha modulator
- Cyclofenil Estrogen receptor modulator
- Dienestrol Estrogen receptor alpha agonist
- Diethylstilbestrol Estrogen receptor alpha agonist
- Diethylstilbestrol diphosphate Estrogen receptor agonist
- Droloxifene Estrogen receptor modulator
- Elacestrant Estrogen receptor alpha degrader
- Elacestrant hydrochloride Estrogen receptor alpha degrader
- Enclomiphene Estrogen receptor alpha modulator