Structure of PDB 3dkf Chain A

Receptor sequence
>3dkfA (length=294) Species: 9606 (Homo sapiens) [Search protein sequence]
TVHIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLKK
IHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPL
VVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKFLASKKFVHRD
LAARNCMLDEKFTVKVADFGLARDMYKLPVKWMALESLQTQKFTTKSDVW
SFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVML
KCWHPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVKE
3D structure
PDB3dkf SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo.
ChainA
Resolution1.8 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D1204 A1206 R1208 N1209 D1222
Catalytic site (residue number reindexed from 1) D150 A152 R154 N155 D168
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 SX8 A I1084 A1108 L1157 Y1159 M1160 D1164 R1208 M1211 A1221 D1222 Y1230 I35 A54 L103 Y105 M106 D110 R154 M157 A167 D168 Y176 MOAD: Ki=2.7nM
PDBbind-CN: -logKd/Ki=8.57,Ki=2.7nM
BindingDB: IC50=4.0nM,Kd=0.820000nM
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:3dkf, PDBe:3dkf, PDBj:3dkf
PDBsum3dkf
PubMed19934279
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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