Structure of PDB 4mxc Chain A

Receptor sequence
>4mxcA (length=290) Species: 9606 (Homo sapiens) [Search protein sequence]
HIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDND
GKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEG
SPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFV
HRDLAARNCMLDEKFTVKVADFGLARDMYDKEYYSVAKLPVKWMALESLQ
TQKFTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPE
YCPDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFIG
3D structure
PDB4mxc Discovery of Anilinopyrimidines as Dual Inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and Cellular Activity
ChainA
Resolution1.632 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 A187
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 DWF A I1084 V1092 A1108 K1110 E1127 M1131 F1134 Y1159 M1160 G1163 D1164 F1200 M1211 A1221 D1222 F1223 I33 V41 A57 K59 E76 M80 F83 Y108 M109 G112 D113 F149 M160 A170 D171 F172 PDBbind-CN: -logKd/Ki=8.17,IC50=6.7nM
BindingDB: IC50=6.7nM
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:4mxc, PDBe:4mxc, PDBj:4mxc
PDBsum4mxc
PubMed24944742
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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