Binding Site Information of Target

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Target General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T92057 Target Info
Target Name Erbb4 tyrosine kinase receptor (Erbb-4)
Synonyms Tyrosine kinase-type cell surface receptor HER4; Receptor tyrosine-protein kinase erbB-4; Proto-oncogene-like protein c-ErbB-4; P180erbB4; HER4
Target Type Successful Target
Gene Name ERBB4
Biochemical Class Kinase
UniProt ID
ERBB4_HUMAN
Drug Binding Sites of Target  Top
Ligand Name: Lapatinib Ligand Info
Structure Description crystal structure of the ErbB4 kinase in complex with lapatinib PDB:3BBT
Method X-ray diffraction Resolution 2.80 Å Mutation No [1]
PDB Sequence
AQLRILKETE
692
LKRVKVLGSG
702
AFGTVYKGIW
712
VPEGETVKIP
722
VAIKILNEGP
734

KANVEFMDEA
744
LIMASMDHPH
754
LVRLLGVCLS
764
PTIQLVTQLM
774
PHGCLLEYVH
784

EHKDNIGSQL
794
LLNWCVQIAK
804
GMMYLEERRL
814
VHRDLAARNV
824
LVKSPNHVKI
834

TDFGLARLLP
858
IKWMALECIH
868
YRKFTHQSDV
878
WSYGVTIWEL
888
MTFGGKPYDG
898

IPTREIPDLL
908
EKGERLPQPP
918
ICTIDVYMVM
928
VKCWMIDADS
938
RPKFKELAAE
948

FSRMARDPQR
958
YLVIQDDRMK
969
LPSP
Residue
Distance (Å)
LEU699
4.129
VAL707
3.488
ALA724
3.216
ILE725
3.849
LYS726
3.390
MET747
3.607
VAL756
4.158
ARG757
4.654
LEU758
3.926
LEU769
3.252
VAL770
4.700
THR771
3.494
Residue
Distance (Å)
GLN772
4.950
LEU773
3.861
MET774
3.307
GLY777
3.505
CYS778
4.191
LEU825
3.459
THR835
3.052
ASP836
3.356
PHE837
2.482
GLY838
4.597
LEU839
3.777
Ligand Name: N-{3-Chloro-4-[(3-Fluorobenzyl)oxy]phenyl}-6-Ethylthieno[3,2-D]pyrimidin-4-Amine Ligand Info
Structure Description ErbB4 kinase domain complexed with a thienopyrimidine inhibitor PDB:2R4B
Method X-ray diffraction Resolution 2.40 Å Mutation No [2]
PDB Sequence
LVEPLTPSGT
703
APNQAQLRIL
713
KETELKRVKV
723
LGSGAFGTVY
733
KGIWVPEGET
743

VKIPVAIKIL
753
NANVEFMDEA
769
LIMASMDHPH
779
LVRLLGVCLS
789
PTIQLVTQLM
799

PHGCLLEYVH
809
EHKDNIGSQL
819
LLNWCVQIAK
829
GMMYLEERRL
839
VHRDLAARNV
849

LVKSPNHVKI
859
TDFGLARLLE
869
GDEKEYNADG
879
GKMPIKWMAL
889
ECIHYRKFTH
899

QSDVWSYGVT
909
IWELMTFGGK
919
PYDGIPTREI
929
PDLLEKGERL
939
PQPPICTIDV
949

YMVMVKCWMI
959
DADSRPKFKE
969
LAAEFSRMAR
979
DPQRYLVIQG
989
DD
Residue
Distance (Å)
LEU724
4.051
VAL732
3.703
ALA749
3.341
ILE750
4.331
LYS751
3.571
MET772
3.844
VAL781
3.587
ARG782
3.505
LEU783
3.238
LEU794
3.195
VAL795
4.142
Residue
Distance (Å)
THR796
3.448
GLN797
3.331
LEU798
3.699
MET799
2.914
GLY802
3.682
CYS803
2.326
LEU850
3.509
THR860
3.401
ASP861
3.298
PHE862
3.470
LEU864
3.984
References  Top
REF 1 Mechanism of activation and inhibition of the HER4/ErbB4 kinase. Structure. 2008 Mar;16(3):460-7.
REF 2 6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases. Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):2773-8.

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