> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/target/ednra-89941d39-d02d-5fd8-ae9f-905322fa3386
> Record changed: 2026-10-13

# EDNRA

ENSG00000151617

Target class

GPCR

Chromosome

4

Approved drugs

7

Clinical candidates (approved and in development)

16

## Clinical evidence

**Approved drugs**

7

**Clinical candidates (approved and in development)**

16

## Druggability

**Chemical probe available**

Yes

## Names

**Target name**

EDNRA

**Gene name**

Endothelin receptor type A

**Gene symbol**

EDNRA

**Protein name**

Endothelin-1 receptor (Endothelin receptor type A) (ET-A) (ETA-R) (hET-AR)

### Other names (3)

- ET-A
- ETA-R
- hET-AR

## Classification

**Gene biotype**

Protein coding

**Gene family**

Endothelin receptors

**Target class**

GPCR

**Target type**

Human gene

## Expression and localisation

**Tissues expressed in**

48

**Protein localisation evidence grade**

Approved

**Highest tissue expression**

89.68

**Tissue specificity (Gini)**

0.644

**Tissue specificity (tau)**

0.859

## Pathways and interactions

**KEGG gene identifiers**

- hsa:1909

**Protein interaction confidence**

0.862625

**Protein interaction partners**

24

### Reactome pathways (2)

- R-HSA-375276
- R-HSA-416476

## Genomic location

**End position**

147544954

**Start position**

147480917

**Chromosome**

4

**Strand**

Forward

## Identifiers

**Ensembl gene ID**

ENSG00000151617

**HGNC ID**

HGNC:3179

Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:3179)

**NCBI Gene ID**

1909

**UniProt ID**

P25101

## Cellular location

- Cell membrane
- Multi-pass membrane protein.
- Plasma membrane

## Tissue expression

**Tissue specificity (tau)**

0.85893

**Expression inequality (Gini)**

0.644218

### Highest expression

Expression in transcripts per million

**Cervix - Ectocervix**

89.68

**Cervix - Endocervix**

82.21

**Uterus**

55.63

**Ovary**

50.4

**Fallopian Tube**

43.67

### All tissues (54)

Expression in transcripts per million

- Cervix - Ectocervix89.68
- Cervix - Endocervix82.21
- Uterus55.63
- Ovary50.4
- Fallopian Tube43.67
- Vagina43.44
- Artery - Tibial38.32
- Artery - Coronary34.58
- Lung31.12
- Prostate30.37
- Bladder23.97
- Heart - Atrial Appendage19.58
- Adipose - Subcutaneous19.25
- Nerve - Tibial18.88
- Artery - Aorta16.65
- Thyroid14.74
- Breast - Mammary Tissue14.43
- Adipose - Visceral (Omentum)11.83
- Minor Salivary Gland9.73
- Esophagus - Gastroesophageal Junction8.58
- Spleen8.08
- Skin - Sun Exposed (Lower leg)7.56
- Skin - Not Sun Exposed (Suprapubic)6.6
- Kidney - Medulla6.52
- Testis6.46

And 29 more, listed on the interactive page.

## Biological functions

### Biological processes (11)

- GO:0006874  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0006874)
- GO:0006939  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0006939)
- GO:0007165  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007165)
- GO:0007190  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007190)
- GO:0007200  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007200)
- GO:0007204  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007204)
- GO:0008283  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0008283)
- GO:0014824  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0014824)
- GO:0042310  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0042310)
- GO:0141156  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0141156)
- GO:2001259  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:2001259)

### Cellular components

- GO:0005886  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005886)

### Molecular functions (2)

- GO:0004435  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0004435)
- GO:0005515  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005515)

## On-target safety

- vasoconstriction  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - clinical: vasoconstriction  
### Biological samples

  - cardiovascular system  
Evidence source  
Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2)
- glomerular and tubulointerstitial structural injury  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: glomerular and tubulointerstitial structural injury  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- teratogenicity  
### Effects

  - Inhibition/Decrease/Downregulation: developmental toxicity  
### Studies

  - clinical: teratogenicity  
### Biological samples

  - cardiovascular system  
Evidence source  
Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2)
- increased aldosterone secretion  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased aldosterone secretion  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased cell proliferation  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased cell proliferation  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- abnormal face  
### Effects

  - Inhibition/Decrease/Downregulation: developmental toxicity  
### Studies

  - preclinical: abnormal face  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased heart rate  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: increased heart rate  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased urine excretion  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: decreased urine excretion  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased cardiac contractility  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased cardiac contractility  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- cardiac anomaly  
### Effects

  - Inhibition/Decrease/Downregulation: developmental toxicity  
### Studies

  - preclinical: cardiac anomaly  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased intestinal transit  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: decreased intestinal transit  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- aldosterone secretion  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - clinical: aldosterone secretion  
### Biological samples

  - cardiovascular system  
Evidence source  
Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2)
- chromosome 22 deletions  
### Effects

  - Inhibition/Decrease/Downregulation: developmental toxicity  
### Studies

  - preclinical: chromosome 22 deletions  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- bronchoconstriction  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: bronchoconstriction  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- pulmonary left ventricular hypertrophy  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: pulmonary left ventricular hypertrophy  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased blood pressure  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased blood pressure  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased heart rate  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: decreased heart rate  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- cleft palate  
### Effects

  - Inhibition/Decrease/Downregulation: developmental toxicity  
### Studies

  - preclinical: cleft palate  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased pain  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased pain  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased gastric emptying  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: decreased gastric emptying  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- osteoblast proliferation  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - clinical: osteoblast proliferation  
### Biological samples

  - cardiovascular system  
Evidence source  
Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2)
- thymic hypoplasia  
### Effects

  - Inhibition/Decrease/Downregulation: developmental toxicity  
### Studies

  - preclinical: thymic hypoplasia  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased pain  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: decreased pain  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased blood pressure  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: decreased blood pressure  
### Biological samples (4)

  - nervous system
  - renal
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- bronchoconstriction  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - clinical: bronchoconstriction  
### Biological samples

  - cardiovascular system  
Evidence source  
Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2)

## Off-target safety

- osteoblast proliferation  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: osteoblast proliferation  
### Biological samples (2)

  - cardiovascular system
  - development  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- receptor binding  
### Studies

  - biochemical: NVS\_GPCR\_hETA, is one of one assay component(s) measured or calculated from the NVS\_GPCR\_hETA assay. It is designed to make measurements of radioligand binding, a form of binding reporter, as detected with scintillation counting signals by Filter-based radiodetection technology.  
### Biological samples

  - cell-free  
Evidence source  
Source: [www.epa.gov](https://www.epa.gov/chemical-research/exploring-toxcast-data-downloadable-data)
- increased blood pressure  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: increased blood pressure  
### Biological samples (2)

  - cardiovascular system
  - development  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- teratogenicity  
### Effects

  - Inhibition/Decrease/Downregulation: developmental toxicity  
### Studies

  - preclinical: teratogenicity  
### Biological samples (2)

  - cardiovascular system
  - development  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- aldosterone secretion  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: aldosterone secretion  
### Biological samples (2)

  - cardiovascular system
  - development  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)

## Related records

### Trials (361)

- : Vascular Function in Health and Disease
- (ARTEMIS-IPF) Randomized, Placebo-Controlled Study to Evaluate Safety and Effectiveness of Ambrisentan in IPF
- (RIGHT HEART III Study - Right Ventricular Hemodynamic Evaluation and Response to Treatment)
- 10mg ZD4054 (Zibotentan) PK Study in Male, Elderly Chinese Patients With Advanced Solid Malignancies
- A 12 Week Safety And Efficacy Study Of Sitaxentan Sodium In Japanese Pulmonary Arterial Hypertension Patients
- A 2-part Study to Investigate the Effect of Macitentan in Healthy Male Participants
- A Clinical Study to Evaluate the Effects of Darusentan on Safety and Efficacy in Subjects With Resistant Systolic Hypertension Receiving Combination Therapy With Three or More Blood Pressure Lowering Drugs
- A Clinical Study to Find Out if Macitentan is Effective and Safe in Japanese Patients With Chronic Thromboembolic Pulmonary Hypertension (CTEPH).
- A Clinical Study to Investigate the Long-term Safety of the Drug Macitentan in Patients With Pulmonary Hypertension Who Were Previously Treated With Macitentan in Clinical Studies.
- A Clinical Trial of Ambrisentan and Tadalafil in Pulmonary Arterial Hypertension Associated With Systemic Sclerosis
- A Drug-drug Interaction Trial in Healthy Female Participants to Investigate the Effect of Aprocitentan on Combined Hormonal Contraceptives
- A Long Term Safety Study With Atrasentan
- A Long Term Study of Ambrisentan in Pulmonary Arterial Hypertension Subjects Having Completed AMB-320 (NCT00423748) or AMB-321 (NCT00423202)
- A Long Term Study to Find Out if Macitentan is an Effective and Safe Treatment for Patients With Heart Failure With Preserved Ejection Fraction and Pulmonary Vascular Disease
- A Long-Term, Open-Label Study to Evaluate the Safety of Sitaxsentan Sodium Treatment in Patients With Pulmonary Arterial Hypertension
- A Non-Interventional, Patient Registry For The Collection Of Pre-Defined Safety Data In Patients Prescribed Thelin
- A Open Label Study to Assess the Long-term Safety, Tolerability and Efficacy of Ambrisentan in Subjects With Inoperable Chronic Thromboembolic Pulmonary Hypertension (CTEPH)
- A Pharmacokinetic Drug-Drug Interaction (DDI) Study Between Sitaxsentan And Sildenafil, And Between Sitaxsentan And Tadalafil After Multiple Doses
- A Phase 1 Relative Bioavailability Study of Ambrisentan and Tadalfil Fixed Dose Combination Tablets in Healthy Subjects
- A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study to Assess Safety and Efficacy of Ambrisentan in Subjects With Pulmonary Arterial Hypertension.

### Drugs (17)

- Ambrisentan Endothelin receptor, ET-A/ET-B antagonist
- Aprocitentan Endothelin receptor, ET-A/ET-B antagonist
- Atrasentan Endothelin receptor ET-A antagonist
- Atrasentan hydrochloride Endothelin receptor ET-A antagonist
- Avosentan Endothelin receptor ET-A antagonist
- Bosentan Endothelin receptor, ET-A/ET-B antagonist
- BQ-123 Endothelin receptor ET-A antagonist
- Clazosentan Endothelin receptor ET-A antagonist
- Darusentan Endothelin receptor ET-A antagonist
- Enrasentan Endothelin receptor ET-A antagonist
- Macitentan Endothelin receptor, ET-A/ET-B antagonist
- Nebentan Endothelin receptor ET-A antagonist
- Sitaxentan Endothelin receptor, ET-A/ET-B antagonist
- Sitaxentan sodium Endothelin receptor, ET-A/ET-B antagonist
- Sparsentan Endothelin receptor ET-A antagonist
- Tezosentan Endothelin receptor ET-A antagonist
- [Zibotentan](https://trialight.com/data/asset/zibotentan-f4c9c1df-415a-4617-939f-43a7b5eda0ea.md) Endothelin receptor ET-A antagonist

---

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