Structure of PDB 5eyc Chain A

Receptor sequence

>5eycA (length=288) Species: 9606 (Homo sapiens)

IDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLKIHC
AVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPLVVL
PYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAA
RNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQT
QKFTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEY
CPDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFI

3D structure

• PDB: 5eyc 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.
• Chain: A
• Resolution: 1.8 Å

Enzymatic activity

• Catalytic site (original residue number in PDB): D1204 A1206 R1208 N1209 D1222 A1243
• Catalytic site (residue number reindexed from 1): D147 A149 R151 N152 D165 A186
• 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	5SZ	A	I1084 V1092 A1108 Y1159 M1160 D1164 R1208 N1209 M1211 A1221 D1222 Y1230	I32 V40 A51 Y102 M103 D107 R151 N152 M154 A164 D165 Y173	MOAD: ic50=3nM PDBbind-CN: -logKd/Ki=8.52,IC50=3nM BindingDB: IC50=3nM

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

External links

• PDB: RCSB:5eyc, PDBe:5eyc, PDBj:5eyc
• PDBsum: 5eyc
• PubMed: 26812066
• UniProt: P08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)