EDNRA
ENSG00000151617
Target class
GPCR
Chromosome
4
Approved drugs
7
Clinical candidates (approved and in development)
16
- Approved drugs
- 7
- Clinical candidates (approved and in development)
- 16
- Chemical probe available
- Yes
- 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)
- ET-A
- ETA-R
- hET-AR
- Gene biotype
- Protein coding
- Gene family
- Endothelin receptors
- Target class
- GPCR
- Target type
- Human gene
- Tissues expressed in
- 48
- Protein localisation evidence grade
- Approved
- Highest tissue expression
- 89.68
- Tissue specificity (Gini)
- 0.644
- Tissue specificity (tau)
- 0.859
- KEGG gene identifiers
- hsa:1909
- Protein interaction confidence
- 0.862625
- Protein interaction partners
- 24
- R-HSA-375276
- R-HSA-416476
- End position
- 147544954
- Start position
- 147480917
- Chromosome
- 4
- Strand
- Forward
- Cell membrane
- Multi-pass membrane protein.
- Plasma membrane
- Tissue specificity (tau)
- 0.85893
- Expression inequality (Gini)
- 0.644218
Expression in transcripts per million
- Cervix - Ectocervix
- 89.68
- Cervix - Endocervix
- 82.21
- Uterus
- 55.63
- Ovary
- 50.4
- Fallopian Tube
- 43.67
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.
- GO:0006874
- GO:0006939
- GO:0007165
- GO:0007190
- GO:0007200
- GO:0007204
- GO:0008283
- GO:0014824
- GO:0042310
- GO:0141156
- GO:2001259
Cellular components
- GO:0005886
- GO:0004435
- GO:0005515
vasoconstriction
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: vasoconstriction
Biological samples
- cardiovascular system
Evidence sourceglomerular and tubulointerstitial structural injury
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: glomerular and tubulointerstitial structural injury
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264teratogenicity
Effects
- Inhibition/Decrease/Downregulation: developmental toxicity
Studies
- clinical: teratogenicity
Biological samples
- cardiovascular system
Evidence sourceincreased aldosterone secretion
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: increased aldosterone secretion
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264increased cell proliferation
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: increased cell proliferation
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264abnormal face
Effects
- Inhibition/Decrease/Downregulation: developmental toxicity
Studies
- preclinical: abnormal face
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264increased heart rate
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: increased heart rate
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264decreased urine excretion
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: decreased urine excretion
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264increased cardiac contractility
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: increased cardiac contractility
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264cardiac anomaly
Effects
- Inhibition/Decrease/Downregulation: developmental toxicity
Studies
- preclinical: cardiac anomaly
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264decreased intestinal transit
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: decreased intestinal transit
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264aldosterone secretion
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: aldosterone secretion
Biological samples
- cardiovascular system
Evidence sourcechromosome 22 deletions
Effects
- Inhibition/Decrease/Downregulation: developmental toxicity
Studies
- preclinical: chromosome 22 deletions
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264bronchoconstriction
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: bronchoconstriction
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264pulmonary left ventricular hypertrophy
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: pulmonary left ventricular hypertrophy
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264increased blood pressure
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: increased blood pressure
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264decreased heart rate
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased heart rate
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264cleft palate
Effects
- Inhibition/Decrease/Downregulation: developmental toxicity
Studies
- preclinical: cleft palate
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264increased pain
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: increased pain
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264decreased gastric emptying
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: decreased gastric emptying
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264osteoblast proliferation
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: osteoblast proliferation
Biological samples
- cardiovascular system
Evidence sourcethymic hypoplasia
Effects
- Inhibition/Decrease/Downregulation: developmental toxicity
Studies
- preclinical: thymic hypoplasia
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264decreased pain
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: decreased pain
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264decreased blood pressure
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: decreased blood pressure
- nervous system
- renal
- cardiovascular
- gastrointestinal
PubMed 28216264bronchoconstriction
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: bronchoconstriction
Biological samples
- cardiovascular system
Evidence source
osteoblast proliferation
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: osteoblast proliferation
- cardiovascular system
- development
PubMed 23197038receptor 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 sourceincreased blood pressure
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: increased blood pressure
- cardiovascular system
- development
PubMed 23197038teratogenicity
Effects
- Inhibition/Decrease/Downregulation: developmental toxicity
Studies
- preclinical: teratogenicity
- cardiovascular system
- development
PubMed 23197038aldosterone secretion
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: aldosterone secretion
- cardiovascular system
- development
PubMed 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 Endothelin receptor ET-A antagonist