DGIdb - EPHA2 Gene Record

EPHA2 1969 Druggable Genome

Alternate Names:

1969
EPH RECEPTOR A2
EPHA2
ARCC2
CTPA
CTPP1
CTRCT6
ECK
176946
3386
ENSG00000142627
OTTHUMG00000009527
P29317
EPHA2_HUMAN
EPHRIN TYPE-A RECEPTOR 2 PRECURSOR (EC 2.7.1.112) (TYROSINE-PROTEIN KINASE RECEPTOR ECK) (EPITHELIAL CELL KINASE). [SOURCE:UNIPROT/SWISSPROT;ACC:P29317]
Tyrosine-protein kinase receptor ECK
Epithelial cell kinase
Ephrin type-A receptor 2
BE0000841
1822
NM_004431
NP_004422
T57278

Gene Info:

Target Subclass	Kinase
Target Subclass	Eph
Transmembrane Helix Count	1
Target Main Class	Receptors
Human Readable Name	DRUGGABLE GENOME
Interpro Short Name	Ser-Thr/Tyr_kinase_cat_dom
Human Readable Name	KINASE
Interpro Acc	IPR001245
Interpro Type	Domain
Uniprot Status	Swiss-Prot
Uniprot Evidence	1: Evidence at protein level
Interpro Name	Serine-threonine/tyrosine-protein kinase catalytic domain
Target Class	Receptors
Target Subclass	EC:2.7.10.1
GuideToPharmacology Gene Category Name	Type XIII RTKs: Ephrin receptor family
GuideToPharmacology Gene Category ID	327
Gene Biotype	PROTEIN_CODING

(15 More Sources)

Gene Categories: Category Details

CELL SURFACE
KINASE
TYROSINE KINASE
DRUGGABLE GENOME

Publications:

Buettner et al., 2008, Inhibition of Src family kinases with dasatinib blocks migration and invasion of human melanoma cells., Mol. Cancer Res.
Konecny et al., 2009, Activity of the multikinase inhibitor dasatinib against ovarian cancer cells., Br. J. Cancer
Faoro et al., 2010, EphA2 mutation in lung squamous cell carcinoma promotes increased cell survival, cell invasion, focal adhesions, and mammalian target of rapamycin activation., J. Biol. Chem.
Lindauer et al., 2010, Dasatinib., Recent Results Cancer Res.
Wang et al., 2007, Identification of candidate predictive and surrogate molecular markers for dasatinib in prostate cancer: rationale for patient selection and efficacy monitoring., Genome Biol.
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Incerti M et al., 2013, Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor., J Med Chem
Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

LITHOGLYCOCHOLATE EPHA2

Interaction Score: 5.98

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23489211

Sources:
DTC
DASATINIB EPHA2

Interaction Score: 0.56

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
19010823 19861960 20360610 20072833 18047674 17139284 17016423

Sources:
MyCancerGenomeClinicalTrial TEND DTC DoCM TdgClinicalTrial DrugBank ChemblInteractions CGI
DORSOMORPHIN EPHA2

Interaction Score: 0.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
REGORAFENIB EPHA2

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial DrugBank
CHEMBL578061 EPHA2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MLN-8054 EPHA2

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SNS-314 EPHA2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ALISERTIB EPHA2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
OSI-632 EPHA2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB EPHA2

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LINIFANIB EPHA2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TOZASERTIB EPHA2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
R-406 EPHA2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SORAFENIB EPHA2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RG-1530 EPHA2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CYC-116 EPHA2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PF-00562271 EPHA2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ILORASERTIB EPHA2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
FOSTAMATINIB EPHA2

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26516587

Sources:
DrugBank

Ensembl: ENSG00000142627
- Version: 101_38
Alternate Names:

EPHA2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P29317
- Version: 01-August-2011
Alternate Names:

ENSG00000142627 Ensembl Gene Id

1969 Entrez Gene Id

P29317 Uniprot Accession

Gene Info:

Target Subclass Kinase

Target Subclass Eph

Transmembrane Helix Count 1

Publications:
TdgClinicalTrial: P29317
- Version: January-2014
Alternate Names:

EPHA2 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass EC:2.7.10.1

Publications:

RussLampel: ENSG00000142627

Version: 26-July-2011

Alternate Names:

ENSG00000142627 Ensembl Gene Id

EPHA2 Display Id

EPHRIN TYPE-A RECEPTOR 2 PRECURSOR (EC 2.7.1.112) (TYROSINE-PROTEIN KINASE RECEPTOR ECK) (EPITHELIAL CELL KINASE). [SOURCE:UNIPROT/SWISSPROT;ACC:P29317] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

HopkinsGroom: P29317
- Version: 11-September-2012
Alternate Names:

EPHRIN TYPE-A RECEPTOR 2 Uniprot Protein Name

EPHA2 Uniprot Gene Name

ENSG00000142627 Ensembl Gene Id

Gene Info:

Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom

Human Readable Name DRUGGABLE GENOME

Human Readable Name KINASE

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
GuideToPharmacology: 1969
- Version: 29-September-2020
Alternate Names:

3386 HUGO Gene ID

3386 HUGO Gene Symbol

EPH receptor A2 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Type XIII RTKs: Ephrin receptor family

GuideToPharmacology Gene Category ID 327

Publications:

DrugBank: BE0000841

Version: 5.1.7

Alternate Names:

EPHA2 DrugBank Gene Name

P29317 UniProt Accession

1969 Entrez Gene Id

Gene Info:

Publications:

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

CGI: EPHA2

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Buettner et al., 2008, Inhibition of Src family kinases with dasatinib blocks migration and invasion of human melanoma cells., Mol. Cancer Res.

Konecny et al., 2009, Activity of the multikinase inhibitor dasatinib against ovarian cancer cells., Br. J. Cancer

Wang et al., 2007, Identification of candidate predictive and surrogate molecular markers for dasatinib in prostate cancer: rationale for patient selection and efficacy monitoring., Genome Biol.

DoCM: EPHA2

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Faoro et al., 2010, EphA2 mutation in lung squamous cell carcinoma promotes increased cell survival, cell invasion, focal adhesions, and mammalian target of rapamycin activation., J. Biol. Chem.

DTC: EPHA2
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Incerti M et al., 2013, Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor., J Med Chem
HingoraniCasas: ENSG00000142627
- Version: 31-May-2017
Alternate Names:

ENSG00000142627 Gene Symbol

EPHA2 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: ECK
- Version: chembl_23
Alternate Names:

ECK GENE_SYMBOL

EPHA2 GENE_SYMBOL

Ephrin type-A receptor 2 UNIPROT

Gene Info:

Publications:
Pharos: EPHA2
- Version: 03-September-2020
Alternate Names:

Ephrin type-A receptor 2 Gene Name

P29317 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:
GO: EPHA2
- Version: 05-September-2020
Alternate Names:

ECK GO Gene Synonym

Gene Info:

Gene Categories:

CELL SURFACE

Publications:
Tempus: EPHA2
- Version: 11-November-2018
Alternate Names:

EPHA2 Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: EPHA2
- Version: 27-Jun-2013
Alternate Names:

1969 Gene ID

ARCC2 dGene Synonym

CTPA dGene Synonym

Gene Info:

Gene Categories:

KINASE, TYROSINE KINASE

Publications:
TTD: Ephrin type-A receptor 2
- Version: 2020.06.01
Alternate Names:

EPHA2 TTD Gene Abbreviation

T57278 TTD Target ID

Gene Info:

Publications:
ClearityFoundationClinicalTrial: EPHA2
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
MyCancerGenomeClinicalTrial: EPHA2
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:

Clinical Status	preclinical
Pathway	activation
Variant Effect	gain-of-function

Details of the Assay for Interaction	Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Mechanism of Interaction	Ephrin receptor inhibitor
Direct Interaction	yes

ENSG00000142627	Ensembl Gene Id
1969	Entrez Gene Id
P29317	Uniprot Accession

EPHRIN TYPE-A RECEPTOR 2	Uniprot Protein Name
EPHA2	Uniprot Gene Name
ENSG00000142627	Ensembl Gene Id

3386	HUGO Gene ID
3386	HUGO Gene Symbol
EPH receptor A2	HUGO Gene Name

EPHA2	DrugBank Gene Name
P29317	UniProt Accession
1969	Entrez Gene Id

ECK	GENE_SYMBOL
EPHA2	GENE_SYMBOL
Ephrin type-A receptor 2	UNIPROT

antagonist (inhibitory)
inhibitor (inhibitory)

EPHA2 Gene Record

EPHA2 1969 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23489211

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Clinical Status preclinical Pathway activation Variant Effect gain-of-function

PMIDs: 19010823 19861960 20360610 20072833 18047674 17139284 17016423

Sources: MyCancerGenomeClinicalTrial TEND DTC DoCM TdgClinicalTrial DrugBank ChemblInteractions CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Assayed using AMPK heterotrimeric complex containing &alpha;2, &beta;1, &gamma;1 subunits Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality:

n/a

PMIDs:
23489211

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
19010823 19861960 20360610 20072833 18047674 17139284 17016423

Sources:
MyCancerGenomeClinicalTrial TEND DTC DoCM TdgClinicalTrial DrugBank ChemblInteractions CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
26516587

Sources:
DrugBank

Alternate Names:

EPHA2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Alternate Names:

ENSG00000142627 Ensembl Gene Id

1969 Entrez Gene Id

P29317 Uniprot Accession

Gene Info:

Target Subclass Kinase

Target Subclass Eph

Transmembrane Helix Count 1

Alternate Names:

EPHA2 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass EC:2.7.10.1

Alternate Names:

ENSG00000142627 Ensembl Gene Id

EPHA2 Display Id

EPHRIN TYPE-A RECEPTOR 2 PRECURSOR (EC 2.7.1.112) (TYROSINE-PROTEIN KINASE RECEPTOR ECK) (EPITHELIAL CELL KINASE). [SOURCE:UNIPROT/SWISSPROT;ACC:P29317] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Alternate Names:

EPHRIN TYPE-A RECEPTOR 2 Uniprot Protein Name

EPHA2 Uniprot Gene Name

ENSG00000142627 Ensembl Gene Id

Gene Info:

Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom

Human Readable Name DRUGGABLE GENOME

Human Readable Name KINASE

Gene Categories:

KINASE, DRUGGABLE GENOME

Alternate Names:

3386 HUGO Gene ID

3386 HUGO Gene Symbol

EPH receptor A2 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Type XIII RTKs: Ephrin receptor family

GuideToPharmacology Gene Category ID 327

Alternate Names:

EPHA2 DrugBank Gene Name

P29317 UniProt Accession

1969 Entrez Gene Id

Publications:

Faoro et al., 2010, EphA2 mutation in lung squamous cell carcinoma promotes increased cell survival, cell invasion, focal adhesions, and mammalian target of rapamycin activation., J. Biol. Chem.

Publications:

Incerti M et al., 2013, Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor., J Med Chem

Alternate Names:

ENSG00000142627 Gene Symbol

EPHA2 Ensembl Id

Gene Categories:

DRUGGABLE GENOME

Alternate Names:

ECK GENE_SYMBOL

EPHA2 GENE_SYMBOL

Ephrin type-A receptor 2 UNIPROT