Structure of PDB 4deg Chain A

Receptor sequence
>4degA (length=286) Species: 9606 (Homo sapiens) [Search protein sequence]
HIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLKIHC
AVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSPLVVLPYM
KHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAARNC
MLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQTQKF
TTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPD
PLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFIG
3D structure
PDB4deg Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.
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) D1204 A1206 R1208 N1209 D1222 A1243
Catalytic site (residue number reindexed from 1) D144 A146 R148 N149 D162 A183
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 0JJ A I1084 A1108 M1160 D1164 R1208 M1211 A1221 D1222 Y1230 I33 A51 M100 D104 R148 M151 A161 D162 Y170 MOAD: ic50=6nM
PDBbind-CN: -logKd/Ki=8.22,IC50=6nM
BindingDB: IC50=3nM,Ki=3.2nM
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:4deg, PDBe:4deg, PDBj:4deg
PDBsum4deg
PubMed22595176
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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