Structure of PDB 5hor Chain A

Receptor sequence
>5horA (length=247) Species: 9606 (Homo sapiens) [Search protein sequence]
QAVQHVVIGPGCVYHGTLKIHCAVKSVSQFLTEGIIMKDFSHPNVLSLLG
ICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKF
LASKKFVHRDLAARNCMLDEKFTVKVADFGLARDMLPVKWTALESLQTQK
FTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCP
DPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATY
3D structure
PDB5hor Discovery and Pharmacokinetic and Pharmacological Properties of the Potent and Selective MET Kinase Inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844).
ChainA
Resolution2.2 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) D110 A112 R114 N115 D128
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 63K A A1108 L1157 Y1159 M1160 K1161 G1163 D1164 R1208 M1211 A1221 D1222 A23 L63 Y65 M66 K67 G69 D70 R114 M117 A127 D128 MOAD: ic50=6nM
PDBbind-CN: -logKd/Ki=8.22,IC50=6nM
BindingDB: IC50=204nM,Kd=0.900000nM
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:5hor, PDBe:5hor, PDBj:5hor
PDBsum5hor
PubMed27355974
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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