Structure of PDB 5ho6 Chain A

Receptor sequence
>5ho6A (length=240) Species: 9606 (Homo sapiens) [Search protein sequence]
VQAVQHVVIGPCVYHGTLIHCAVKSVSQFLTEGIIMKDFSHPNVLSLLGI
CGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKFLASKK
FVHRDLAARNCMLDEKFTVKVADFGLARLPVKWMALESLQTQKFTTKSDV
WSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVM
LKCWHPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATY
3D structure
PDB5ho6 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
Resolution1.97 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) D105 A107 R109 N110 D123
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 H1162 G1163 D1164 M1211 D1222 A1226 A22 L58 Y60 M61 K62 H63 G64 D65 M112 D123 A127 MOAD: ic50=204nM
PDBbind-CN: -logKd/Ki=6.69,IC50=204nM
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:5ho6, PDBe:5ho6, PDBj:5ho6
PDBsum5ho6
PubMed27355974
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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