Structure of PDB 3f66 Chain A

Receptor sequence
>3f66A (length=288) Species: 9606 (Homo sapiens) [Search protein sequence]
HIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLKIH
CAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPLVV
LPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLA
ARNCMLDEKFTVKVADFGLARDMYDKEYYSVAKLPVKWMALESLQTQKFT
TKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDP
LYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFIGEHY
3D structure
PDB3f66 Discovery of a novel series of quinoxalines as inhibitors of c-Met kinase.
ChainA
Resolution1.4 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) D148 A150 R152 N153 D166 A182
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 IHX A I1084 A1108 L1157 Y1159 M1160 M1211 I33 A52 L101 Y103 M104 M155 MOAD: ic50=0.9uM
PDBbind-CN: -logKd/Ki=6.05,IC50=0.9uM
BindingDB: IC50=900nM
BS02 GBL A M1211 A1221 D1222 Y1230 M155 A165 D166 Y174
BS03 GBL A M1131 L1140 L1142 F1223 G1224 L1225 M75 L84 L86 F167 G168 L169
BS04 GBL A P1176 D1180 F1216 P120 D124 F160
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

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Molecular Function

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Biological Process
External links
PDB RCSB:3f66, PDBe:3f66, PDBj:3f66
PDBsum3f66
PubMed19059779
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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