EPH receptor A7 | Type XIII RTKs: Ephrin receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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EPH receptor A7

Target not currently curated in GtoImmuPdb

Target id: 1827

Nomenclature: EPH receptor A7

Abbreviated Name: EphA7

Family: Type XIII RTKs: Ephrin receptor family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 998 6q16.3 EPHA7 EPH receptor A7
Mouse 1 998 4 Epha7 Eph receptor A7
Rat 1 998 5q21 Epha7 Eph receptor A7
Previous and Unofficial Names
HEK11 | EPH homology kinase 3 | ephrin type-A receptor 7 | tyrosine-protein kinase receptor EHK-3 | EBK | Embryonic brain kinase | MDK1
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Kinase domain of human ephrin type-A receptor 7 (Epha7)
PDB Id:  2REI
Resolution:  1.6Å
Species:  Human
References: 
Image of receptor 3D structure from RCSB PDB
Description:  Complex between the kinase domain of human ephrin type-a receptor 7 (epha7) and inhibitor alw-ii-49-7
PDB Id:  3DKO
Resolution:  2.0Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.10.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
DDR1/2 inhibitor 5n Hs Inhibition 6.7 pKd 7
pKd 6.7 (Kd 2x10-7 M) [7]
compound 8h [PMID: 21561767] Hs Inhibition 8.4 pIC50 6
pIC50 8.4 (IC50 4.2x10-9 M) [6]
compound 66 [PMID: 19788238] Hs Inhibition 5.9 pIC50 5
pIC50 5.9 (IC50 1.118x10-6 M) [5]
compound 20 [PMID: 23489211] Mm Inhibition 5.7 pIC50 4
pIC50 5.7 (IC50 2.1x10-6 M) [4]
View species-specific inhibitor tables
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 2,8

Key to terms and symbols Click column headers to sort
Target used in screen: EPHA7
Ligand Sp. Type Action Value Parameter
foretinib Hs Inhibitor Inhibition 8.6 pKd
tamatinib Hs Inhibitor Inhibition 7.4 pKd
linifanib Hs Inhibitor Inhibition 7.0 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.7 pKd
lestaurtinib Hs Inhibitor Inhibition 6.6 pKd
KW-2449 Hs Inhibitor Inhibition 6.4 pKd
crizotinib Hs Inhibitor Inhibition 6.3 pKd
cediranib Hs Inhibitor Inhibition 6.2 pKd
staurosporine Hs Inhibitor Inhibition 6.2 pKd
doramapimod Hs Inhibitor Inhibition 6.1 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: EphA7/EPHA7
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 11.5 20.5 2.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 14.2 3.0 -2.0
vandetanib Hs Inhibitor Inhibition 31.8
K-252a Hs Inhibitor Inhibition 41.3 32.0 4.0
Syk inhibitor Hs Inhibitor Inhibition 41.3 32.0 9.0
JAK3 inhibitor II Hs Inhibitor Inhibition 46.1 34.0 7.0
sunitinib Hs Inhibitor Inhibition 50.8
compound 56 [PMID: 8568816] Hs Inhibitor Inhibition 58.5 48.0 7.0
Gö 6976 Hs Inhibitor Inhibition 62.6 43.0 39.0
AG1478 Hs Inhibitor Inhibition 65.0 73.0 22.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

3. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

4. Incerti M, Tognolini M, Russo S, Pala D, Giorgio C, Hassan-Mohamed I, Noberini R, Pasquale EB, Vicini P, Piersanti S et al.. (2013) Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor. J. Med. Chem., 56 (7): 2936-47. [PMID:23489211]

5. Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C. (2009) Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4). J. Med. Chem., 52 (20): 6433-46. [PMID:19788238]

6. Thomas M, Huang WS, Wen D, Zhu X, Wang Y, Metcalf CA, Liu S, Chen I, Romero J, Zou D et al.. (2011) Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. Bioorg. Med. Chem. Lett., 21 (12): 3743-8. [PMID:21561767]

7. Wang Z, Zhang Y, Pinkas DM, Fox AE, Luo J, Huang H, Cui S, Xiang Q, Xu T, Xun Q et al.. (2018) Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2. J. Med. Chem., 61 (17): 7977-7990. [PMID:30075624]

8. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Type XIII RTKs: Ephrin receptor family: EPH receptor A7. Last modified on 16/10/2018. Accessed on 21/09/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1827.