Structure of PDB 3l8v Chain A

Receptor sequence
>3l8vA (length=293) Species: 9606 (Homo sapiens) [Search protein sequence]
DLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDNDGK
KIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSP
LVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKFLASKKFVHR
DLAARNCMLDEKFTVKVADFGNKTGAKLPVKWMALESLQTQKFTTKSDVW
SFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVML
KCWHPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVK
3D structure
PDB3l8v Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.
ChainA
Resolution2.4 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) D151 A153 R155 N156 D169 A176
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 L8V A I1084 V1092 A1108 K1110 E1127 M1131 F1134 L1157 M1160 H1202 M1211 V1220 A1221 D1222 F1223 I31 V39 A55 K57 E74 M78 F81 L104 M107 H149 M158 V167 A168 D169 F170 MOAD: ic50=0.008uM
PDBbind-CN: -logKd/Ki=8.10,IC50=8nM
BindingDB: IC50=8nM
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:3l8v, PDBe:3l8v, PDBj:3l8v
PDBsum3l8v
PubMed20382527
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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