Tchem EPHA1 Ephrin type-A receptor 1

Protein Summary

Description

Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Binds with a low affinity EFNA3 and EFNA4 and with a high affinity to EFNA1 which most probably constitutes its cognate/functional ligand. Upon activation by EFNA1 induces cell attachment to the extracellular matrix inhibiting cell spreading and motility through regulation of ILK and downstream RHOA and RAC. Plays also a role in angiogenesis and regulates cell proliferation. May play a role in apoptosis. This gene belongs to the ephrin receptor subfamily of the protein-tyrosine kinase family. EPH and EPH-related receptors have been implicated in mediating developmental events, particularly in the nervous system. Receptors in the EPH subfamily typically have a single kinase domain and an extracellular region containing a Cys-rich domain and 2 fibronectin type III repeats. The ephrin receptors are divided into 2 groups based on the similarity of their extracellular domain sequences and their affinities for binding ephrin-A and ephrin-B ligands. This gene is expressed in some human cancer cell lines and has been implicated in carcinogenesis. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P21709
• A1L3V3
• B5A966
• B5A967
• Q15405
• hEpha1

Gene Name

• EPHA1

Ensembl ID

• ENST00000275815
• ENSP00000275815
• ENSG00000146904
• ENST00000645847
• ENSP00000494931
• ENSG00000284816

Symbol

• EPH
• EPHT
• EPHT1
• EPH
• EPHT
• EPHT1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
protein domain	1
molecular function	0.99
biological process	0.88
PubMedID	0.84
kinase perturbation	0.76

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Eph Family / Ephrin Type-a Receptor 1

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: 660.75   (req: < 5)

Gene RIFs: 39   (req: <= 3)

Antibodies: 539   (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: 660.75   (req: >= 5)

Gene RIFs: 39   (req: > 3)

Antibodies: 539   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 26

Tchem

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

Active Ligands: 10

Tclin

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

Active Drugs: 2

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Expression Data (0 Tissues)

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No expression data found

Related Tools

ProKinO

The ProKinO is a protein kinase-specific ontology, which provides a controlled vocabulary of terms, their hierarchy, and relationships unifying sequence, structure, function, mutation and pathway information on kinases.

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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 (2)

Explore Approved Drugs

1 – 2 of 2

dasatinib

EPHA1Tchem Kinase

INHIBITOR pKd : 7.89

regorafenib

EPHA1Tchem Kinase

INHIBITOR pIC50 : 9.3

Active Ligands (10)

Explore Active Ligands

1 – 10 of 10

foretinib

EPHA1Tchem Kinase

pKd : 7.92

PD-173955

EPHA1Tchem Kinase

pKd : 7.92

XL-228

EPHA1Tchem Kinase

pKd : 7.58

CHEMBL249097

EPHA1Tchem Kinase

pKd : 8.3

CHEMBL566515

EPHA1Tchem Kinase

pIC50 : 9.04

compound 20 [PMID: 23489211]

EPHA1Tchem Kinase

pIC50 : 5.82

saracatinib

EPHA1Tchem Kinase

pKd : 8

Tesevatinib

EPHA1Tchem Kinase

pKd : 8.1

sapitinib

EPHA1Tchem Kinase

pKd : 7.82

CHEMBL450519

EPHA1Tchem Kinase

pKd : 8

Protein-Protein Interactions (226)

Explore Interacting Targets

1 – 10 of 226

• See Interactions on String-DB

SMG1

Tchem

Family:  Kinase

Novelty:  0.00854339

p_int:  0.999999799

p_ni:  2.01e-7

Score:  0.277

Data Source:  BioPlex,STRINGDB

RELCH

Tdark

Novelty:  0.33696386

p_int:  0.9999997

p_ni:  2.99e-7

Score:  0.162

Data Source:  BioPlex,STRINGDB

USP34

Tbio

Family:  Enzyme

Novelty:  0.16444192

p_int:  0.999997791

p_ni:  0.000002209

Score:  0.159

Data Source:  BioPlex,STRINGDB

SMG9

Tbio

Novelty:  0.03940774

p_int:  0.999987991

p_ni:  5.3e-7

p_wrong:  0.000011479

Score:  0.187

Data Source:  BioPlex,STRINGDB

FAM114A2

Tdark

Novelty:  0.40545319

p_int:  0.999981741

p_ni:  0.00001824

p_wrong:  1.9e-8

Data Source:  BioPlex

DYNC2H1

Tbio

Novelty:  0.01306616

p_int:  0.999980059

p_ni:  0.000019941

Score:  0.188

Data Source:  BioPlex,STRINGDB

DIAPH3

Tbio

Novelty:  0.01165283

p_int:  0.99997974

p_ni:  0.00002026

Score:  0.159

Data Source:  BioPlex,STRINGDB

GSDME

Tbio

Novelty:  0.01231123

p_int:  0.999979601

p_ni:  0.000020399

Data Source:  BioPlex

KIF14

Tbio

Novelty:  0.02313641

p_int:  0.999976879

p_ni:  0.000023121

Score:  0.257

Data Source:  BioPlex,STRINGDB

WDR13

Tbio

Novelty:  0.05397678

p_int:  0.999973179

p_ni:  0.000001948

p_wrong:  0.000024873

Score:  0.2

Data Source:  BioPlex,STRINGDB

Nearest Tclin Targets (1)

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Downstream (1)

1 – 1 of 1

ABL1

Tclin

Family:  Kinase

KEGG Distance:  1

Common Pathways:  1

1: Axon guidance

Pathways (9)

Reactome (6)

KEGG (1)

PathwayCommons (2)

Axon guidance (R-HSA-422475)

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Find Similar Targets

Items per page:

5

1 – 5 of 6

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Axon guidance	533 targets	R-HSA-422475
Reactome	Developmental Biology	1055 targets	R-HSA-1266738
Reactome	EPH-Ephrin signaling	92 targets	R-HSA-2682334
Reactome	EPH-ephrin mediated repulsion of cells	49 targets	R-HSA-3928665
Reactome	POU5F1 (OCT4), SOX2, NANOG activate genes related to proliferation	13 targets	R-HSA-2892247

Name	Explore in Pharos	Explore in Source
Axon guidance	533 targets	R-HSA-422475
Developmental Biology	1055 targets	R-HSA-1266738
EPH-Ephrin signaling	92 targets	R-HSA-2682334
EPH-ephrin mediated repulsion of cells	49 targets	R-HSA-3928665
POU5F1 (OCT4), SOX2, NANOG activate genes related to proliferation	13 targets	R-HSA-2892247

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (31)

Functions (6)

Components (5)

Processes (20)

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Items per page:

10

1 – 6 of 6

GO Term	Evidence	Assigned by
protein kinase activity	Inferred from Direct Assay (IDA)	UniProtKB
transmembrane-ephrin receptor activity	Inferred from Direct Assay (IDA)	UniProtKB
protein kinase binding	Inferred from Physical Interaction (IPI)	UniProtKB
transmembrane receptor protein tyrosine kinase activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
transmembrane signaling receptor activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
ATP binding	Inferred from Electronic Annotation (IEA)	UniProtKB-KW

Disease Associations ()

No disease associations found

GWAS Traits (16)

Items per page:

5

1 – 5 of 16

GWAS Trait	EFO ID	ENSG ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
serum gamma-glutamyl transferase measurement	EFO_0004532	ENSG00000146904	2	2	2		89.2
serum gamma-glutamyl transferase measurement	EFO_0004532	ENSG00000284816	2	2	2		89.2
basophil count	EFO_0005090	ENSG00000284816	3	1	3		85.2
basophil count	EFO_0005090	ENSG00000146904	3	1	3		85.2
basophil percentage of leukocytes	EFO_0007992	ENSG00000146904	1	1	1		84.9

Items per page:

5

1 – 5 of 16

GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
serum gamma-glutamyl transferase measurement	EFO_0004532	2		89.2
serum gamma-glutamyl transferase measurement	EFO_0004532	2		89.2
basophil count	EFO_0005090	3		85.2
basophil count	EFO_0005090	3		85.2
basophil percentage of leukocytes	EFO_0007992	1		84.9

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UniProt Keyword Find Similar Targets

No Header	No Header
3D-structure
Alternative splicing
Angiogenesis
ATP-binding
Cell adhesion
Cell membrane
Complete proteome
Glycoprotein
Kinase
Membrane

GWAS Trait Find Similar Targets

No Header	No Header
Alzheimer's disease
basophil count
basophil percentage of leukocytes
family history of Alzheimer’s disease
monocyte count
monocyte percentage of leukocytes
serum gamma-glutamyl transferase measurement
sex hormone-binding globulin measurement

MGI Phenotype Find Similar Targets

No Header	No Header
growth/size/body region phenotype
homeostasis/metabolism phenotype
immune system phenotype
limbs/digits/tail phenotype
reproductive system phenotype

IDG Resources

No IDG generated resources found

Orthologs (10)

1 – 5 of 10

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	EPH receptor A1	VGNC:14442	463808
Mouse	Eph receptor A1	MGI:107381	13835
Rat	Eph receptor A1	RGD:1304680	312279
Dog	EPH receptor A1	VGNC:40404	482735
Horse	EPH receptor A1	VGNC:17616	100056221

Species	Name	OMA	EggNOG	Inparanoid
Chimp	EPH receptor A1
Mouse	Eph receptor A1
Rat	Eph receptor A1
Dog	EPH receptor A1
Horse	EPH receptor A1

Publication Statistics

PubMed Score 660.75

PubMed score by year

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PubTator Score 135.90

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Patents

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Related Publications

Text Mined References (61)

GeneRif Annotations (39)

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PMID	Year	Title