EPH receptor A1

Target id: 1821

Nomenclature: EPH receptor A1

Abbreviated Name: EphA1

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

   GtoImmuPdb view: OFF :     Currently no data for EPH receptor A1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 976 7q32-q36 EPHA1 EPH receptor A1
Mouse 1 977 6 Epha1 Eph receptor A1
Rat - 977 4q23 Epha1 Eph receptor A1
Previous and Unofficial Names
EPHT1 | ephrin type-A receptor 1 | Embryonic stem cell kinase | tyrosine-protein kinase receptor ESK | Esk
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
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:  SAM Domain of Human Ephrin Type-A Receptor 1 (EphA1)
PDB Id:  3HIL
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 Affinity Units Reference
compound 66 [PMID: 19788238] Hs Inhibition 8.5 pIC50 5
pIC50 8.5 (IC50 2.9x10-9 M) [5]
compound 20 [PMID: 23489211] Hs Inhibition 5.6 pIC50 4
pIC50 5.6 (IC50 2.3x10-6 M) [4]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: EPHA1
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 8.4 pKd
foretinib Hs Inhibitor Inhibition 8.2 pKd
PD-173955 Hs Inhibitor Inhibition 8.2 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.4 pKd
tamatinib Hs Inhibitor Inhibition 7.2 pKd
PP-242 Hs Inhibitor Inhibition 7.0 pKd
crizotinib Hs Inhibitor Inhibition 6.8 pKd
KW-2449 Hs Inhibitor Inhibition 6.8 pKd
vandetanib Hs Inhibitor Inhibition 6.6 pKd
staurosporine Hs Inhibitor Inhibition 6.5 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: EphA1/EPHA1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Hs Inhibitor Inhibition 2.7
PP1 analog II Hs Inhibitor Inhibition 29.8 7.0 -1.0
staurosporine Hs Inhibitor Inhibition 31.0 3.0 -2.0
TWS119 Hs Inhibitor Inhibition 31.2 2.0 -1.0
dorsomorphin Hs Inhibitor Inhibition 31.4 17.0 1.0
vandetanib Hs Inhibitor Inhibition 31.7
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 37.4 1.0 3.0
IKK-2 inhibitor IV Hs Inhibitor Inhibition 56.6 9.0 6.0
K-252a Hs Inhibitor Inhibition 62.6 3.0 0.0
nilotinib Hs Inhibitor Inhibition 63.2
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. 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 A1. Last modified on 11/02/2015. Accessed on 12/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1821.