Tchem EPHA1 Ephrin type-A receptor 1

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Eph Family / 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

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: 1191.45   (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: 1191.45   (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: 6

Tclin

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

Active Drug: 1

Approved Drugs (1)

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1 – 1 of 1

dasatinib

EPHA1Tchem Kinase

Kd: 8.39

Active Ligands (6)

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1 – 6 of 6

CHEMBL1230609

EPHA1Tchem Kinase

Kd: 8.21

CHEMBL386051

EPHA1Tchem Kinase

Kd: 8.19

CHEMBL566515

EPHA1Tchem Kinase

IC50: 8.54

CHEMBL249097

EPHA1Tchem Kinase

Kd: 8.3

compound 20 [PMID: 23489211]

EPHA1Tchem Kinase

IC50: 5.63999987

CHEMBL450519

EPHA1Tchem Kinase

Kd: 8

Protein Data Bank (4)

1 – 4 of 4

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

PDB Structure Id	M.W.	Resolution	Pub Year

Pathways (9)

Reactome (6)

KEGG (1)

PathwayCommons (2)

Axon guidance (R-HSA-422475)

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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

Gene Ontology Terms (31)

Functions (6)

Components (5)

Processes (20)

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

Protein-Protein Interactions (226)

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1 – 10 of 226

• See Interactions on String-DB

SMG1

Tchem

Family: Kinase

Novelty: 0.01292797

p_int: 0.999999799

p_ni: 2.01e-7

Score: 0.277

Data Source: BioPlex,STRINGDB

RELCH

Tdark

Novelty: 0.49441458

p_int: 0.9999997

p_ni: 2.99e-7

Score: 0.162

Data Source: BioPlex,STRINGDB

USP34

Tbio

Family: Enzyme

Novelty: 0.34090909

p_int: 0.999997791

p_ni: 0.000002209

Score: 0.159

Data Source: BioPlex,STRINGDB

SMG9

Tbio

Novelty: 0.01309043

p_int: 0.999987991

p_ni: 5.3e-7

p_wrong: 0.000011479

Score: 0.187

Data Source: BioPlex,STRINGDB

FAM114A2

Tdark

Novelty: 0.75

p_int: 0.999981741

p_ni: 0.00001824

p_wrong: 1.9e-8

Data Source: BioPlex

DYNC2H1

Tbio

Novelty: 0.02553321

p_int: 0.999980059

p_ni: 0.000019941

Score: 0.188

Data Source: BioPlex,STRINGDB

DIAPH3

Tbio

Novelty: 0.01662716

p_int: 0.99997974

p_ni: 0.00002026

Score: 0.159

Data Source: BioPlex,STRINGDB

GSDME

Tbio

Novelty: 0.01946224

p_int: 0.999979601

p_ni: 0.000020399

Data Source: BioPlex

KIF14

Tbio

Novelty: 0.02907785

p_int: 0.999976879

p_ni: 0.000023121

Score: 0.257

Data Source: BioPlex,STRINGDB

WDR13

Tbio

Novelty: 0.04399633

p_int: 0.999973179

p_ni: 0.000001948

p_wrong: 0.000024873

Score: 0.2

Data Source: BioPlex,STRINGDB

Publication Statistics

PubMed Score  1191.45

PubMed score by year

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PubTator Score  135.9

PubTator score by year

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Patents

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Amino Acid Sequence

Residue Counts

Sequence

MERRWPLGLGLVLLLCAPLPPGARAKEVTLMDTSKAQGELGWLLDPPKDGWSEQQQILNGTPLYMYQDCP

1-70

MQGRRDTDHWLRSNWIYRGEEASRVHVELQFTVRDCKSFPGGAGPLGCKETFNLLYMESDQDVGIQLRRP

70-140

LFQKVTTVAADQSFTIRDLVSGSVKLNVERCSLGRLTRRGLYLAFHNPGACVALVSVRVFYQRCPETLNG

140-210

LAQFPDTLPGPAGLVEVAGTCLPHARASPRPSGAPRMHCSPDGEWLVPVGRCHCEPGYEEGGSGEACVAC

210-280

PSGSYRMDMDTPHCLTCPQQSTAESEGATICTCESGHYRAPGEGPQVACTGPPSAPRNLSFSASGTQLSL

280-350

RWEPPADTGGRQDVRYSVRCSQCQGTAQDGGPCQPCGVGVHFSPGARGLTTPAVHVNGLEPYANYTFNVE

350-420

AQNGVSGLGSSGHASTSVSISMGHAESLSGLSLRLVKKEPRQLELTWAGSRPRSPGANLTYELHVLNQDE

420-490

ERYQMVLEPRVLLTELQPDTTYIVRVRMLTPLGPGPFSPDHEFRTSPPVSRGLTGGEIVAVIFGLLLGAA

490-560

LLLGILVFRSRRAQRQRQQRQRDRATDVDREDKLWLKPYVDLQAYEDPAQGALDFTRELDPAWLMVDTVI

560-630

GEGEFGEVYRGTLRLPSQDCKTVAIKTLKDTSPGGQWWNFLREATIMGQFSHPHILHLEGVVTKRKPIMI

630-700

ITEFMENGALDAFLREREDQLVPGQLVAMLQGIASGMNYLSNHNYVHRDLAARNILVNQNLCCKVSDFGL

700-770

TRLLDDFDGTYETQGGKIPIRWTAPEAIAHRIFTTASDVWSFGIVMWEVLSFGDKPYGEMSNQEVMKSIE

770-840

DGYRLPPPVDCPAPLYELMKNCWAYDRARRPHFQKLQAHLEQLLANPHSLRTIANFDPRMTLRLPSLSGS

840-910

DGIPYRTVSEWLESIRMKRYILHFHSAGLDTMECVLELTAEDLTQMGITLPGHQKRILCSIQGFKD

910-976

MERRWPLGLGLVLLLCAPLPPGARAKEVTLMDTSKAQGELGWLLDPPKDGWSEQQQILNGTPLYMYQDCPMQGRRDTDHWLRSNWIYRGEEASRVHVELQFTVRDCKSFPGGAGPLGCKETFNLLYMESDQDVGIQLRRPLFQKVTTVAADQSFTIRDLVSGSVKLNVERCSLGRLTRRGLYLAFHNPGACVALVSVRVFYQRCPETLNGLAQFPDTLPGPAGLVEVAGTCLPHARASPRPSGAPRMHCSPDGEWLVPVGRCHCEPGYEEGGSGEACVACPSGSYRMDMDTPHCLTCPQQSTAESEGATICTCESGHYRAPGEGPQVACTGPPSAPRNLSFSASGTQLSLRWEPPADTGGRQDVRYSVRCSQCQGTAQDGGPCQPCGVGVHFSPGARGLTTPAVHVNGLEPYANYTFNVEAQNGVSGLGSSGHASTSVSISMGHAESLSGLSLRLVKKEPRQLELTWAGSRPRSPGANLTYELHVLNQDEERYQMVLEPRVLLTELQPDTTYIVRVRMLTPLGPGPFSPDHEFRTSPPVSRGLTGGEIVAVIFGLLLGAALLLGILVFRSRRAQRQRQQRQRDRATDVDREDKLWLKPYVDLQAYEDPAQGALDFTRELDPAWLMVDTVIGEGEFGEVYRGTLRLPSQDCKTVAIKTLKDTSPGGQWWNFLREATIMGQFSHPHILHLEGVVTKRKPIMIITEFMENGALDAFLREREDQLVPGQLVAMLQGIASGMNYLSNHNYVHRDLAARNILVNQNLCCKVSDFGLTRLLDDFDGTYETQGGKIPIRWTAPEAIAHRIFTTASDVWSFGIVMWEVLSFGDKPYGEMSNQEVMKSIEDGYRLPPPVDCPAPLYELMKNCWAYDRARRPHFQKLQAHLEQLLANPHSLRTIANFDPRMTLRLPSLSGSDGIPYRTVSEWLESIRMKRYILHFHSAGLDTMECVLELTAEDLTQMGITLPGHQKRILCSIQGFKD

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Uniprot Keyword

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