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EPH receptor A6

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Target id: 1826

Nomenclature: EPH receptor A6

Abbreviated Name: EphA6

Family: Type XIII RTKs: Ephrin receptor family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1036 3q11.2 EPHA6 EPH receptor A6
Mouse 1 1035 16 C1.3 Epha6 Eph receptor A6
Rat 1 1035 11q12 Epha6 Eph receptor A6
Previous and Unofficial Names Click here for help
EHK2 | EPH homology kinase 2 | ephrin type-A receptor 6 | tyrosine-protein kinase receptor EHK-2 | Hek12
Database Links Click here for help
Alphafold Q9UF33 (Hs), Q62413 (Mm), P54758 (Rn)
BRENDA 2.7.10.1
CATH/Gene3D 2.60.120.260, 2.60.40.10
ChEMBL Target CHEMBL4526 (Hs), CHEMBL4739690 (Mm)
Ensembl Gene ENSG00000080224 (Hs), ENSMUSG00000055540 (Mm), ENSRNOG00000029184 (Rn)
Entrez Gene 285220 (Hs), 13840 (Mm), 29202 (Rn)
Human Protein Atlas ENSG00000080224 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:285220 (Hs), mmu:13840 (Mm), rno:29202 (Rn)
OMIM 600066 (Hs)
Pharos Q9UF33 (Hs)
RefSeq Nucleotide NM_001080448 (Hs), NM_007938 (Mm), XM_221595 (Rn)
RefSeq Protein NP_001073917 (Hs), NP_031964 (Mm), XP_221595 (Rn)
UniProtKB Q9UF33 (Hs), Q62413 (Mm), P54758 (Rn)
Wikipedia EPHA6 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.10.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 20 [PMID: 23489211] Small molecule or natural product Click here for species-specific activity table Mm Inhibition 5.8 pIC50 3
⤷ pIC50 5.8 (IC50 1.5x10-6 M) [3]
DiscoveRx KINOMEscan® screen Click here for help
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: 2,4
Key to terms and symbols Click column headers to sort
Target used in screen: EPHA6
Ligand Sp. Type Action Value Parameter
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 7.4 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.9 pKd
brivanib Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
canertinib Small molecule or natural product Immunopharmacology Ligand 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 Click here for help
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
Key to terms and symbols Click column headers to sort
Target used in screen: nd/EPHA6
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 3.3
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 4.4
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6
PP1 analog II Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.4
SU11274 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 24.0
AG1478 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 27.8
gefitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 28.9
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 29.5
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 30.2
PDGF RTK inhibitor Small molecule or natural product Hs Inhibitor Inhibition 33.0
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. 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]

4. 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 A6. Last modified on 09/02/2015. Accessed on 04/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1826.