Structure of PDB 3cth Chain A

Receptor sequence
>3cthA (length=295) Species: 9606 (Homo sapiens) [Search protein sequence]
HIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDND
GKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEG
SPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKFLASKKFV
HRDLAARNCMLDEKFTVKVADFGNKTGAKLPVKWMALESLQTQKFTTKSD
VWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEV
MLKCWHPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVK
3D structure
PDB3cth Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors
ChainA
Resolution2.3 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) D153 A155 R157 N158 D171 A178
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 319 A A1108 K1110 E1127 M1131 F1134 L1157 Y1159 M1160 H1202 M1211 A1221 D1222 F1223 A57 K59 E76 M80 F83 L106 Y108 M109 H151 M160 A170 D171 F172 MOAD: ic50=0.035uM
PDBbind-CN: -logKd/Ki=6.96,IC50=0.11uM
BindingDB: IC50=35nM
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:3cth, PDBe:3cth, PDBj:3cth
PDBsum3cth
PubMed18479916
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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