Structure of PDB 2vwu Chain A

Receptor sequence
>2vwuA (length=253) Species: 9606 (Homo sapiens) [Search protein sequence]
EIDVSYVKIEEVIGAGEFGEVCRGRLKAPGKKESCVAIKTLTERQRREFL
SEASIMGQFEHPNIIRLEGVVTNSMPVMILTEFMENGALDSFLRLNDGQF
TVIQLVGMLRGIASGMRYLAEMSYVHRDLAARNILVNSNLVCKVSDFIPI
RWTAPEAIAFRKFTSASDAWSYGIVMWEVMSFGERPYWDMSNQDVINAIE
QDYRLPPPPDCPTSLHQLMLDCWQKDRNARPRFPQVVSALDKMIRNPASL
KIV
3D structure
PDB2vwu Inhibitors of the Tyrosine Kinase Ephb4. Part 1: Structure-Based Design and Optimization of a Series of 2,4-Bis-Anilinopyrimidines
ChainA
Resolution2.0 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D740 A742 R744 N745 D758 P783
Catalytic site (residue number reindexed from 1) D128 A130 R132 N133 D146 P149
Enzyme Commision number 2.7.10.1: receptor protein-tyrosine kinase.
Interaction with ligand
Site
#
Ligand Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01 7X1 A I621 A645 K647 E664 I691 T693 M696 E697 G699 L747 S757 I13 A37 K39 E52 I79 T81 M84 E85 G87 L135 S145 MOAD: ic50=0.35uM
PDBbind-CN: -logKd/Ki=6.46,IC50=0.35uM
BindingDB: IC50=350nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:2vwu, PDBe:2vwu, PDBj:2vwu
PDBsum2vwu
PubMed18434142
UniProtP54760|EPHB4_HUMAN Ephrin type-B receptor 4 (Gene Name=EPHB4)

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