Target Binding Site Detail

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Target General Information
Ligand General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T28413 Target Info
Target Name Ephrin type-A receptor 3 (EPHA3)
Synonyms hEK4; Tyrosineprotein kinase receptor ETK1; Tyrosineprotein kinase TYRO4; Tyrosine-protein kinase receptor ETK1; Tyrosine-protein kinase TYRO4; TYRO4; Human embryo kinase; HEK; Ephrin typeA receptor 3; Ephlike tyrosine kinase 1; Eph-like tyrosine kinase 1; ETK1; ETK protein; EPHlike kinase 4; EPH-like kinase 4; EK4
Target Type Clinical trial Target
Gene Name EPHA3
Biochemical Class Kinase
UniProt ID
EPHA3_HUMAN
Ligand General Information  Top
Ligand Name Phosphonotyrosine Ligand Info
Canonical SMILES C1=CC(=CC=C1CC(C(=O)O)N)OP(=O)(O)O
InChI 1S/C9H12NO6P/c10-8(9(11)12)5-6-1-3-7(4-2-6)16-17(13,14)15/h1-4,8H,5,10H2,(H,11,12)(H2,13,14,15)/t8-/m0/s1
InChIKey DCWXELXMIBXGTH-QMMMGPOBSA-N
PubChem Compound ID 30819
Drug Binding Sites of Target  Top
PDB ID: 2QO7      Human EphA3 kinase and juxtamembrane region, dephosphorylated, AMP-PNP bound
Method X-ray diffraction Resolution 1.60 Å Mutation No [1]
PDB Sequence
TYVDPHTVHE
611
FAKELDATNI
621
SIDKVVGAGE
631
FGEVCSGRLK
641
LPSKKEISVA
651

IKTLKVGYTE
661
KQRRDFLGEA
671
SIMGQFDHPN
681
IIRLEGVVTK
691
SKPVMIVTEM
702

ENGSLDSFLR
712
KHDAQFTVIQ
722
LVGMLRGIAS
732
GMKYLSDMGY
742
VHRDLAARNI
752

LINSNLVCKV
762
SDFGPIRWTS
792
PEAIAYRKFT
802
SASDVWSYGI
812
VLWEVMSYGE
822

RPYWEMSNQD
832
VIKAVDEGYR
842
LPPPMDCPAA
852
LYQLMLDCWQ
862
KDRNNRPKFE
872

QIVSILDKLI
882
RNPGSLKIIT
892
SPSNLLLD
Residue
Distance (Å)
ASP624
4.368
LYS625
2.323
SER637
3.554
SER649
3.374
VAL650
3.659
ALA651
4.023
Residue
Distance (Å)
THR699
3.490
GLU700
1.326
MET702
1.332
GLU703
3.600
ASN755
4.601
PDB ID: 2QOQ      Human EphA3 kinase and juxtamembrane region, base, AMP-PNP bound structure
Method X-ray diffraction Resolution 1.60 Å Mutation No [1]
PDB Sequence
TYVDPHEDPT
606
QTVHEFAKEL
616
DATNISIDKV
626
VGAGEFGEVC
636
SGRLKLPSKK
646

EISVAIKTLK
656
VGYTEKQRRD
666
FLGEASIMGQ
676
FDHPNIIRLE
686
GVVTKSKPVM
696

IVTEMENGSL
707
DSFLRKHDAQ
717
FTVIQLVGML
727
RGIASGMKYL
737
SDMGYVHRDL
747

AARNILINSN
757
LVCKVSDFGK
785
IPIRWTSPEA
795
IAYRKFTSAS
805
DVWSYGIVLW
815

EVMSYGERPY
825
WEMSNQDVIK
835
AVDEGYRLPP
845
PMDCPAALYQ
855
LMLDCWQKDR
865

NNRPKFEQIV
875
SILDKLIRNP
885
GSLKIITNLL
902
LDQS
Residue
Distance (Å)
ASP624
4.456
LYS625
3.725
SER637
3.787
SER649
3.416
VAL650
3.624
ALA651
4.046
Residue
Distance (Å)
THR699
3.469
GLU700
1.324
MET702
1.330
GLU703
3.583
ASN755
4.617
PDB ID: 3FXX      Human EphA3 Kinase and Juxtamembrane Region Bound to Substrate KQWDNYE[pTyr]IW
Method X-ray diffraction Resolution 1.70 Å Mutation Yes [2]
PDB Sequence
TQTVHEFAKE
615
LDATNISIDK
625
VVGAGEFGEV
635
CSGRLKLPSK
645
KEISVAIKTL
655

KVGYTEKQRR
665
DFLGEASIMG
675
QFDHPNIIRL
685
EGVVTKSKPV
695
MIVTEYMENG
705

SLDSFLRKHD
715
AQFTVIQLVG
725
MLRGIASGMK
735
YLSDMGYVHR
745
DLAARNILIN
755

SNLVCKVSDF
765
GLSRVLEDDG
784
KIPIRWTSPE
794
AIAYRKFTSA
804
SDVWSYGIVL
814

WEVMSYGERP
824
YWEMSNQDVI
834
KAVDEGYRLP
844
PPMDCPAALY
854
QLMLDCWQKD
864

RNNRPKFEQI
874
VSILDKLIRN
884
PGSLKIITAA
896
RPSNLLLD
Residue
Distance (Å)
GLY784
3.369
LYS785
3.475
Residue
Distance (Å)
ILE786
4.911
ILE788
3.896
References  Top
REF 1 Autoregulation by the juxtamembrane region of the human ephrin receptor tyrosine kinase A3 (EphA3). Structure. 2008 Jun;16(6):873-84.
REF 2 Structural recognition of an optimized substrate for the ephrin family of receptor tyrosine kinases. FEBS J. 2009 Aug;276(16):4395-404.

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