Tclin EDNRA Endothelin-1 receptor

Protein Summary

Description

Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3. This gene encodes the receptor for endothelin-1, a peptide that plays a role in potent and long-lasting vasoconstriction. This receptor associates with guanine-nucleotide-binding (G) proteins, and this coupling activates a phosphatidylinositol-calcium second messenger system. Polymorphisms in this gene have been linked to migraine headache resistance. Alternative splicing results in multiple transcript variants. [provided by RefSeq, Oct 2009]

Uniprot Accession IDs

• P25101
• B2R723
• B4E2V6
• B7Z9G6
• D3DP03
• E7ER36
• O43441
• Q16432
• Q16433
• Q8TBH2

Gene Name

• EDNRA

Ensembl ID

• ENST00000324300
• ENSP00000315011
• ENSG00000151617
• ENST00000358556
• ENSP00000351359
• ENST00000506066
• ENSP00000425281
• ENST00000510697
• ENSP00000427259
• ENST00000511804
• ENSP00000425354
• ENST00000648866
• ENSP00000496976

Symbol

• ETA
• ETRA
• ETA
• ET-A
• ETAR
• ETRA
• MFDA
• ETA-R
• hET-AR

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
biological term	0.92
transcription factor perturbation	0.84
chemical	0.82
disease	0.81

Protein Classes

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Endothelin Receptor / Endothelin Type A / Endothelin-1 Receptor

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1978.13   (req: < 5)

Gene RIFs: 147   (req: <= 3)

Antibodies: 326   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1978.13   (req: >= 5)

Gene RIFs: 147   (req: > 3)

Antibodies: 326   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 22

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 831

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 4

Expression Data (0 Tissues)

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No expression data found

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Related Tools (4)

Target Illumination GWAS Analytics (TIGA)

TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.

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GENEVA

GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.

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GlyGen

GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.

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ARCHS4

ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.

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Approved Drugs (4)

Explore Approved Drugs

1 – 4 of 4

bosentan

EDNRATclin GPCR

ANTAGONIST pKi : 7.1

sitaxentan

EDNRATclin GPCR

ANTAGONIST pKi : 9.37

macitentan

EDNRATclin GPCR

ANTAGONIST pIC50 : 6.41

ambrisentan

EDNRATclin GPCR

ANTAGONIST pKi : 9.65

Active Ligands (831)

Explore Active Ligands

1 – 10 of 831

CHEMBL4128926

EDNRATclin GPCR

pKd : 9.92

CHEMBL372814

EDNRATclin GPCR

pIC50 : 7.89

CHEMBL278176

EDNRATclin GPCR

pIC50 : 7.89

sparsentan

EDNRATclin GPCR

pKi : 8.03

aprocitentan

EDNRATclin GPCR

pIC50 : 8.47

atrasentan

EDNRATclin GPCR

pKi : 10.47

darusentan

EDNRATclin GPCR

pKi : 8.22

SB209670

EDNRATclin GPCR

pKi : 9.37

Endothelin-1

EDNRATclin GPCR

pIC50 : 10

CHEMBL325581

EDNRATclin GPCR

pIC50 : 10.15

Protein-Protein Interactions (244)

Explore Interacting Targets

1 – 10 of 244

• See Interactions on String-DB

BCL2L11

Tchem

Novelty:  0.00055914

p_int:  0.994878599

p_ni:  0.005121396

p_wrong:  5e-9

Score:  0.553

Data Source:  BioPlex,STRINGDB

MCL1

Tchem

Novelty:  0.00046181

p_int:  0.980366422

p_ni:  0.019633577

p_wrong:  1e-9

Score:  0.561

Data Source:  BioPlex,STRINGDB

MTX1

Tbio

Novelty:  0.02350764

p_int:  0.97084787

p_ni:  0.02915213

Score:  0.181

Data Source:  BioPlex,STRINGDB

ARL5B

Tbio

Family:  Enzyme

Novelty:  0.03703395

p_int:  0.941469891

p_ni:  0.058510427

p_wrong:  0.000019682

Score:  0.19

Data Source:  BioPlex,STRINGDB

LMBR1

Tbio

Novelty:  0.00591824

p_int:  0.902245521

p_ni:  0.096104913

p_wrong:  0.001649566

Score:  0.187

Data Source:  BioPlex,STRINGDB

MT-ND1

Tclin

Family:  Enzyme

Novelty:  0.00090183

p_int:  0.875744027

p_ni:  0.097652729

p_wrong:  0.026603245

Score:  0.175

Data Source:  BioPlex,STRINGDB

EBP

Tchem

Family:  Enzyme

Novelty:  0.00610658

p_int:  0.861392487

p_ni:  0.137217551

p_wrong:  0.001389961

Score:  0.211

Data Source:  BioPlex,STRINGDB

SYNGR2

Tbio

Novelty:  0.1089664

p_int:  0.860654258

p_ni:  0.13932102

p_wrong:  0.000024722

Score:  0.211

Data Source:  BioPlex,STRINGDB

MT-CO1

Tchem

Family:  Enzyme

Novelty:  0.00008262

p_int:  0.798530801

p_ni:  0.201451169

p_wrong:  0.00001803

Score:  0.181

Data Source:  BioPlex,STRINGDB

EDN1

Tbio

Novelty:  0.00007453

Score:  0.999

Data Source:  Reactome,STRINGDB

Nearest Tclin Targets

Nearest Tclin calculations are only available for targets with KEGG Pathway annotations.

Pathways (23)

Reactome (7)

KEGG (7)

PathwayCommons (3)

WikiPathways (6)

Class A/1 (Rhodopsin-like receptors) (R-HSA-373076)

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1 – 5 of 7

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Class A/1 (Rhodopsin-like receptors)	323 targets	R-HSA-373076
Reactome	G alpha (q) signalling events	219 targets	R-HSA-416476
Reactome	GPCR downstream signalling	1152 targets	R-HSA-388396
Reactome	GPCR ligand binding	460 targets	R-HSA-500792
Reactome	Peptide ligand-binding receptors	189 targets	R-HSA-375276

Name	Explore in Pharos	Explore in Source
Class A/1 (Rhodopsin-like receptors)	323 targets	R-HSA-373076
G alpha (q) signalling events	219 targets	R-HSA-416476
GPCR downstream signalling	1152 targets	R-HSA-388396
GPCR ligand binding	460 targets	R-HSA-500792
Peptide ligand-binding receptors	189 targets	R-HSA-375276

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (24)

Functions (2)

Components (2)

Processes (20)

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1 – 2 of 2

GO Term	Evidence	Assigned by
phosphatidylinositol phospholipase C activity	Traceable Author Statement (TAS)	ProtInc
endothelin receptor activity	Non-traceable Author Statement (NAS)	UniProtKB

Disease Associations (null)

No disease associations found

GWAS Traits (10)

• Explore on Target Illumination GWAS Analytics (TIGA)

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5

1 – 5 of 10

GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
coronary artery disease	EFO_0001645	6	5	4	1.1	95.9
brain aneurysm	EFO_0003870	3	3	2	1.2	89.8
platelet crit	EFO_0007985	2	2	2		88
platelet count	EFO_0004309	1	1	1		71
red blood cell density measurement	EFO_0007978	1	1	1		59.6

• Explore on Target Illumination GWAS Analytics (TIGA)

Items per page:

5

1 – 5 of 10

GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
coronary artery disease	EFO_0001645	4	1.1	95.9
brain aneurysm	EFO_0003870	2	1.2	89.8
platelet crit	EFO_0007985	2		88
platelet count	EFO_0004309	1		71
red blood cell density measurement	EFO_0007978	1		59.6

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Find similar targets by:

UniProt Keyword Find Similar Targets

No Header	No Header
Alternative splicing
Cell membrane
Complete proteome
Disease mutation
Disulfide bond
G-protein coupled receptor
Glycoprotein
Membrane
Phosphoprotein
Polymorphism

GWAS Trait Find Similar Targets

No Header	No Header
brain aneurysm
carotid atherosclerosis
coronary artery disease
hematocrit
hemoglobin measurement
myocardial infarction
peripheral arterial disease
platelet count
platelet crit
red blood cell density measurement

MGI Phenotype Find Similar Targets

No Header	No Header
behavior/neurological phenotype
cardiovascular system phenotype
cellular phenotype
craniofacial phenotype
digestive/alimentary phenotype
embryo phenotype
endocrine/exocrine gland phenotype
growth/size/body region phenotype
hearing/vestibular/ear phenotype
hematopoietic system phenotype

IDG Resources

No IDG generated resources found

Orthologs (14)

1 – 5 of 14

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	endothelin receptor type A	VGNC:594	461530
Macaque	endothelin receptor type A		704135
Mouse	endothelin receptor type A	MGI:105923	13617
Rat	endothelin receptor type A	RGD:2535	24326
Dog	endothelin receptor type A	VGNC:40202	450187

Species	Name	OMA	EggNOG	Inparanoid
Chimp	endothelin receptor type A
Macaque	endothelin receptor type A
Mouse	endothelin receptor type A
Rat	endothelin receptor type A
Dog	endothelin receptor type A

Publication Statistics

PubMed Score 1978.13

PubMed score by year

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PubTator Score 2210.99

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Patents

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Related Publications

GeneRif Annotations (147)

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PMID	Text