Structure of PDB 3ctj Chain A

Receptor sequence
>3ctjA (length=289) Species: 9606 (Homo sapiens) [Search protein sequence]
VHIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDN
DGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSE
GSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKFLASKKF
VHRDLAARNCMLDEKFTVKVADFLPVKWMALESLQTQKFTTKSDVWSFGV
LLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCWH
PKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVK
3D structure
PDB3ctj Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors
ChainA
Resolution2.5 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) D154 A156 R158 N159 D172
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 320 A A1108 M1131 L1157 Y1159 M1160 M1211 V1220 A1221 D1222 F1223 A58 M81 L107 Y109 M110 M161 V170 A171 D172 F173 MOAD: ic50=0.11uM
PDBbind-CN: -logKd/Ki=7.46,IC50=0.035uM
BindingDB: IC50=110nM
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:3ctj, PDBe:3ctj, PDBj:3ctj
PDBsum3ctj
PubMed18479916
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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