EPH receptor A8 | Type XIII RTKs: Ephrin receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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EPH receptor A8

Target not currently curated in GtoImmuPdb

Target id: 1828

Nomenclature: EPH receptor A8

Abbreviated Name: EphA8

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 1 495 1p36.12 EPHA8 EPH receptor A8
Mouse 1 1004 4 Epha8 Eph receptor A8
Rat - 978 5q36 Epha8 Eph receptor A8
Previous and Unofficial Names
HEK3 | EPH- and ELK-related kinase | ephrin type-A receptor 8 | tyrosine-protein kinase receptor EEK
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
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 8 (EPHA8)
PDB Id:  3KUL
Resolution:  2.15Å
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 7.1 pKd 7
pKd 7.1 (Kd 7.9x10-8 M) [7]
compound 66 [PMID: 19788238] Hs Inhibition 8.4 pIC50 6
pIC50 8.4 (IC50 4.5x10-9 M) [6]
RIPK3 inhibitor 18 Hs Inhibition 7.6 pIC50 4
pIC50 7.6 (IC50 2.6x10-8 M) [4]
compound 20 [PMID: 23489211] Mm Inhibition 5.8 pIC50 5
pIC50 5.8 (IC50 1.5x10-6 M) [5]
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: EPHA8
Ligand Sp. Type Action Value Parameter
dasatinib Hs Inhibitor Inhibition 9.6 pKd
foretinib Hs Inhibitor Inhibition 8.7 pKd
PD-173955 Hs Inhibitor Inhibition 8.2 pKd
bosutinib Hs Inhibitor Inhibition 8.1 pKd
AST-487 Hs Inhibitor Inhibition 7.7 pKd
nilotinib Hs Inhibitor Inhibition 7.4 pKd
vandetanib Hs Inhibitor Inhibition 7.0 pKd
staurosporine Hs Inhibitor Inhibition 6.7 pKd
PP-242 Hs Inhibitor Inhibition 6.6 pKd
doramapimod Hs Inhibitor Inhibition 6.6 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: EphA8/EPHA8
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Hs Inhibitor Inhibition 4.1
bosutinib Hs Inhibitor Inhibition 10.5
staurosporine Hs Inhibitor Inhibition 25.7 29.5 9.0
nilotinib Hs Inhibitor Inhibition 28.4
vandetanib Hs Inhibitor Inhibition 33.9
TWS119 Hs Inhibitor Inhibition 57.5 30.0 6.0
PP1 analog II Hs Inhibitor Inhibition 66.8 33.0 6.0
tozasertib Hs Inhibitor Inhibition 77.1
SC-68376 Hs Inhibitor Inhibition 78.8 65.0 54.0
dorsomorphin Hs Inhibitor Inhibition 79.8 90.0 41.0
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. Hart AC, Abell L, Guo J, Mertzman ME, Padmanabha R, Macor JE, Chaudhry C, Lu H, O'Malley K, Shaw PJ et al.. (2019) Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage. ACS Med Chem Lett, Article ASAP. DOI: 10.1021/acsmedchemlett.9b00065

5. 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]

6. 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]

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 A8. Last modified on 17/05/2019. Accessed on 12/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1828.