Binding Site Information of Target

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Target General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T56121 Target Info
Target Name Ephrin type-B receptor 3 (EPHB3)
Synonyms hEK2; Tyrosine-protein kinase TYRO6; TYRO6; Embryonic kinase 2; ETK2; EPH-like tyrosine kinase 2; EPH-like kinase 2; EK2
Target Type Literature-reported Target
Gene Name EPHB3
Biochemical Class Kinase
UniProt ID
EPHB3_HUMAN
Drug Binding Sites of Target  Top
Ligand Name: 1-(4-Anilinoquinazolin-7-yl)ethanone Ligand Info
Structure Description EphB3 kinase domain covalently bound to an irreversible inhibitor (compound 3) PDB:5L6O
Method X-ray diffraction Resolution 1.88 Å Mutation Yes [1]
PDB Sequence
CVKIEEVIGA
641
GEVCRGRLKQ
654
PGRREVFVAI
664
KTLKVGYTER
674
QRRDFLSEAS
684

IMGQFDHPNI
694
IRLEGVVTKS
704
RPVMILTEFM
714
ENCALDSFLR
724
LNDGQFTVIQ
734

LVGMLRGIAA
744
GMKYLSEMNY
754
VHRDLAARNI
764
LVNSNLVCKV
774
SDFGLEDDPS
788

DPTYTSSLGG
798
KIPIRWTAPE
808
AIAYRKFTSA
818
SDVWSYGIVM
828
WEVMSYGERP
838

YWDMSNQDVI
848
NAVEQDYRLP
858
PPMDCPTALH
868
QLMLDCWVRD
878
RNLRPKFSQI
888

VNTLDKLIRN
898
PASLKVI
Residue
Distance (Å)
ILE639
3.319
VAL647
3.669
ALA663
3.372
LYS665
3.556
MET686
3.615
ILE695
4.142
ILE709
3.812
THR711
3.115
GLU712
3.389
PHE713
3.734
Residue
Distance (Å)
MET714
3.185
GLU715
4.091
ASN716
4.576
CYS717
1.818
LEU765
3.499
SER775
3.743
ASP776
3.490
PHE777
4.009
GLY778
4.011
Ligand Name: N-(4-anilinoquinazolin-7-yl)acetamide Ligand Info
Structure Description EphB3 kinase domain covalently bound to an irreversible inhibitor (compound 6) PDB:5L6P
Method X-ray diffraction Resolution 2.26 Å Mutation Yes [1]
PDB Sequence
CVKIEEVIGA
641
GEFGEVCRGR
651
LKQPGRREVF
661
VAIKTLKVGY
671
TERQRRDFLS
681

EASIMGQFDH
691
PNIIRLEGVV
701
TKSRPVMILT
711
EFMENCALDS
721
FLRLNDGQFT
731

VIQLVGMLRG
741
IAAGMKYLSE
751
MNYVHRDLAA
761
RNILVNSNLV
771
CKVSDFGLSR
781

FLEDDPSDPT
791
YTSSLGGKIP
801
IRWTAPEAIA
811
YRKFTSASDV
821
WSYGIVMWEV
831

MSYGERPYWD
841
MSNQDVINAV
851
EQDYRLPPPM
861
DCPTALHQLM
871
LDCWVRDRNL
881

RPKFSQIVNT
891
LDKLIRNPAS
901
LKVI
Residue
Distance (Å)
ILE639
3.883
VAL647
4.274
ALA663
3.521
LYS665
3.477
MET686
3.900
ILE695
4.198
ILE709
4.797
THR711
3.538
GLU712
3.291
Residue
Distance (Å)
PHE713
3.775
MET714
3.006
CYS717
1.821
LEU765
3.587
SER775
3.699
ASP776
3.556
PHE777
3.788
GLY778
3.707
LEU779
4.048
References  Top
REF 1 Development of Specific, Irreversible Inhibitors for a Receptor Tyrosine Kinase EphB3. J Am Chem Soc. 2016 Aug 24;138(33):10554-60.

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