Structure of PDB 4eev Chain A

Receptor sequence
>4eevA (length=283) Species: 9606 (Homo sapiens) [Search protein sequence]
PLLQNTVHIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYH
GTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLG
ICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKY
LASKKFVHRDLAARNCMLDEKFTVKVADFGKLPVKWMALESLQTQKFTTK
SDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLY
EVMLKCWHPKAEMRPSFSELVSRISAIFSTFIG
3D structure
PDB4eev LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models.
ChainA
Resolution1.8 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
Catalytic site (residue number reindexed from 1) D160 A162 R164 N165 D178
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 L1X A I1084 A1108 E1127 M1131 L1157 Y1159 M1160 M1211 V1220 A1221 D1222 F1223 I40 A64 E83 M87 L113 Y115 M116 M167 V176 A177 D178 F179 MOAD: ic50=4.7nM
PDBbind-CN: -logKd/Ki=8.33,IC50=4.7nM
BindingDB: IC50=4.7nM
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

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Molecular Function
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Biological Process
External links
PDB RCSB:4eev, PDBe:4eev, PDBj:4eev
PDBsum4eev
PubMed23275061
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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