Structure of PDB 5eyd Chain A

Receptor sequence
>5eydA (length=289) Species: 9606 (Homo sapiens) [Search protein sequence]
HIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLKIHC
AVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSSPLVVLPY
MKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAARN
CMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQTQK
FTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCP
DPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFIGEH
3D structure
PDB5eyd Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
ChainA
Resolution1.85 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) D145 A147 R149 N150 D163 A184
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 5T1 A I1084 V1092 A1108 Y1159 M1160 D1164 R1208 N1209 M1211 A1221 D1222 Y1230 I33 V41 A51 Y100 M101 D105 R149 N150 M152 A162 D163 Y171 MOAD: ic50=1nM
PDBbind-CN: -logKd/Ki=9.00,IC50=1nM
BindingDB: IC50=1nM
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:5eyd, PDBe:5eyd, PDBj:5eyd
PDBsum5eyd
PubMed26812066
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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