Tchem EPHA3 Ephrin type-A receptor 3

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Eph Family / Ephrin Type-a Receptor 3

Protein Summary

Description

Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin 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. Highly promiscuous for ephrin-A ligands it binds preferentially EFNA5. Upon activation by EFNA5 regulates cell-cell adhesion, cytoskeletal organization and cell migration. Plays a role in cardiac cells migration and differentiation and regulates the formation of the atrioventricular canal and septum during development probably through activation by EFNA1. Involved in the retinotectal mapping of neurons. May also control the segregation but not the guidance of motor and sensory axons during neuromuscular circuit development. 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 encodes a protein that binds ephrin-A ligands. Two alternatively spliced transcript variants have been described for this gene. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P29320
• Q9H2V3
• Q9H2V4

Gene Name

• EPHA3

Ensembl ID

• ENST00000336596
• ENSP00000337451
• ENSG00000044524
• ENST00000452448
• ENSP00000399926

Symbol

• ETK
• ETK1
• HEK
• TYRO4
• EK4
• ETK
• HEK
• ETK1
• HEK4
• TYRO4

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
protein domain	1
molecular function	0.99
transcription factor perturbation	0.94
microRNA	0.93
gene perturbation	0.8

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: 269.4   (req: < 5)

Gene RIFs: 36   (req: <= 3)

Antibodies: 457   (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: 269.4   (req: >= 5)

Gene RIFs: 36   (req: > 3)

Antibodies: 457   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 24

Tchem

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

Active Ligands: 11

Tclin

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

Active Drugs: 2

Approved Drugs (2)

Explore Approved Drugs

1 – 2 of 2

dasatinib

EPHA3Tchem Kinase

Kd: 10.03

bosutinib

EPHA3Tchem Kinase

Kd: 8.24

Active Ligands (11)

Explore Active Ligands

1 – 10 of 11

CHEMBL388978

EPHA3Tchem Kinase

Kd: 7.57

CHEMBL1230609

EPHA3Tchem Kinase

Kd: 9

CHEMBL386051

EPHA3Tchem Kinase

Kd: 8.12

CHEMBL1784637

EPHA3Tchem Kinase

IC50: 8.92000008

CHEMBL566515

EPHA3Tchem Kinase

IC50: 7.4000001

CHEMBL2336005

EPHA3Tchem Kinase

IC50: 8.29

CHEMBL249097

EPHA3Tchem Kinase

Kd: 10

compound 20 [PMID: 23489211]

EPHA3Tchem Kinase

IC50: 5.5999999

sitravatinib

EPHA3Tchem Kinase

IC50: 9

CHEMBL459850

EPHA3Tchem Kinase

EC50: 8.7

Protein Data Bank (27)

1 – 5 of 27

PDB Structure Id	Ligand	Method	Resolution (Å)	M.W. (kDa)	Pub Year	Title

PDB Structure Id	M.W.	Resolution	Pub Year

Pathways (11)

Reactome (4)

KEGG (1)

PathwayCommons (4)

WikiPathways (2)

Axon guidance (R-HSA-422475)

Click on a row in the table to change the structure displayed.

Items per page:

5

1 – 4 of 4

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

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

Gene Ontology Terms (31)

Functions (5)

Components (7)

Processes (19)

Items per page:

10

1 – 5 of 5

GO Term	Evidence	Assigned by
GPI-linked ephrin receptor activity	Inferred from Direct Assay (IDA)	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
transmembrane-ephrin receptor activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
ATP binding	Inferred from Electronic Annotation (IEA)	UniProtKB-KW

Protein-Protein Interactions (134)

Explore Interacting Targets

1 – 10 of 134

• See Interactions on String-DB

EPHA7

Tchem

Family: Kinase

Novelty: 0.01421837

p_int: 0.999935474

p_ni: 0.000064479

p_wrong: 4.7e-8

Score: 0.933

Data Source: BioPlex,STRINGDB

EFNA5

Tbio

Novelty: 0.00173565

p_int: 0.999878385

p_ni: 0.000121615

Score: 0.999

Data Source: BioPlex,STRINGDB

LRRIQ1

Tdark

p_int: 0.99128511

p_ni: 0.008713257

p_wrong: 0.000001632

Score: 0.554

Data Source: BioPlex,STRINGDB

FAM118B

Tdark

Novelty: 2.25

p_int: 0.95513242

p_ni: 0.033751333

p_wrong: 0.011116247

Score: 0.165

Data Source: BioPlex,STRINGDB

SLAMF1

Tbio

Novelty: 0.00121506

p_int: 0.946129735

p_ni: 0.041240495

p_wrong: 0.01262977

Score: 0.157

Data Source: BioPlex,STRINGDB

HLA-DRA

Tbio

Novelty: 0.00705028

p_int: 0.881035982

p_ni: 0.091317198

p_wrong: 0.027646819

Score: 0.181

Data Source: BioPlex,STRINGDB

TMEM231

Tbio

Novelty: 0.22861101

p_int: 0.781509957

p_ni: 0.193004433

p_wrong: 0.025485609

Score: 0.179

Data Source: BioPlex,STRINGDB

CEACAM21

Tdark

Novelty: 0.98765432

p_int: 0.770190719

p_ni: 0.20593599

p_wrong: 0.02387329

Data Source: BioPlex

EFNB2

Tbio

Novelty: 0.00309066

Score: 0.998

Data Source: STRINGDB

EFNB1

Tbio

Novelty: 0.00491089

Score: 0.995

Data Source: STRINGDB

Publication Statistics

PubMed Score  269.40

PubMed score by year

Reset Zoom

PubTator Score  103.27

PubTator score by year

Reset Zoom

Patents

Reset Zoom

Amino Acid Sequence

Residue Counts

Sequence

MDCQLSILLLLSCSVLDSFGELIPQPSNEVNLLDSKTIQGELGWISYPSHGWEEISGVDEHYTPIRTYQV

1-70

CNVMDHSQNNWLRTNWVPRNSAQKIYVELKFTLRDCNSIPLVLGTCKETFNLYYMESDDDHGVKFREHQF

70-140

TKIDTIAADESFTQMDLGDRILKLNTEIREVGPVNKKGFYLAFQDVGACVALVSVRVYFKKCPFTVKNLA

140-210

MFPDTVPMDSQSLVEVRGSCVNNSKEEDPPRMYCSTEGEWLVPIGKCSCNAGYEERGFMCQACRPGFYKA

210-280

LDGNMKCAKCPPHSSTQEDGSMNCRCENNYFRADKDPPSMACTRPPSSPRNVISNINETSVILDWSWPLD

280-350

TGGRKDVTFNIICKKCGWNIKQCEPCSPNVRFLPRQFGLTNTTVTVTDLLAHTNYTFEIDAVNGVSELSS

350-420

PPRQFAAVSITTNQAAPSPVLTIKKDRTSRNSISLSWQEPEHPNGIILDYEVKYYEKQEQETSYTILRAR

420-490

GTNVTISSLKPDTIYVFQIRARTAAGYGTNSRKFEFETSPDSFSISGESSQVVMIAISAAVAIILLTVVI

490-560

YVLIGRFCGYKSKHGADEKRLHFGNGHLKLPGLRTYVDPHTYEDPTQAVHEFAKELDATNISIDKVVGAG

560-630

EFGEVCSGRLKLPSKKEISVAIKTLKVGYTEKQRRDFLGEASIMGQFDHPNIIRLEGVVTKSKPVMIVTE

630-700

YMENGSLDSFLRKHDAQFTVIQLVGMLRGIASGMKYLSDMGYVHRDLAARNILINSNLVCKVSDFGLSRV

700-770

LEDDPEAAYTTRGGKIPIRWTSPEAIAYRKFTSASDVWSYGIVLWEVMSYGERPYWEMSNQDVIKAVDEG

770-840

YRLPPPMDCPAALYQLMLDCWQKDRNNRPKFEQIVSILDKLIRNPGSLKIITSAAARPSNLLLDQSNVDI

840-910

TTFRTTGDWLNGVWTAHCKEIFTGVEYSSCDTIAKISTDDMKKVGVTVVGPQKKIISSIKALETQSKNGP

910-980

VPV

980-983

MDCQLSILLLLSCSVLDSFGELIPQPSNEVNLLDSKTIQGELGWISYPSHGWEEISGVDEHYTPIRTYQVCNVMDHSQNNWLRTNWVPRNSAQKIYVELKFTLRDCNSIPLVLGTCKETFNLYYMESDDDHGVKFREHQFTKIDTIAADESFTQMDLGDRILKLNTEIREVGPVNKKGFYLAFQDVGACVALVSVRVYFKKCPFTVKNLAMFPDTVPMDSQSLVEVRGSCVNNSKEEDPPRMYCSTEGEWLVPIGKCSCNAGYEERGFMCQACRPGFYKALDGNMKCAKCPPHSSTQEDGSMNCRCENNYFRADKDPPSMACTRPPSSPRNVISNINETSVILDWSWPLDTGGRKDVTFNIICKKCGWNIKQCEPCSPNVRFLPRQFGLTNTTVTVTDLLAHTNYTFEIDAVNGVSELSSPPRQFAAVSITTNQAAPSPVLTIKKDRTSRNSISLSWQEPEHPNGIILDYEVKYYEKQEQETSYTILRARGTNVTISSLKPDTIYVFQIRARTAAGYGTNSRKFEFETSPDSFSISGESSQVVMIAISAAVAIILLTVVIYVLIGRFCGYKSKHGADEKRLHFGNGHLKLPGLRTYVDPHTYEDPTQAVHEFAKELDATNISIDKVVGAGEFGEVCSGRLKLPSKKEISVAIKTLKVGYTEKQRRDFLGEASIMGQFDHPNIIRLEGVVTKSKPVMIVTEYMENGSLDSFLRKHDAQFTVIQLVGMLRGIASGMKYLSDMGYVHRDLAARNILINSNLVCKVSDFGLSRVLEDDPEAAYTTRGGKIPIRWTSPEAIAYRKFTSASDVWSYGIVLWEVMSYGERPYWEMSNQDVIKAVDEGYRLPPPMDCPAALYQLMLDCWQKDRNNRPKFEQIVSILDKLIRNPGSLKIITSAAARPSNLLLDQSNVDITTFRTTGDWLNGVWTAHCKEIFTGVEYSSCDTIAKISTDDMKKVGVTVVGPQKKIISSIKALETQSKNGPVPV

Find similar targets by:

Uniprot Keyword

3D-structure
Alternative splicing
ATP-binding
Cell adhesion
Cell membrane
Complete proteome
Direct protein sequencing
Glycoprotein
Kinase
Membrane