Structure of PDB 5hlw Chain A

Receptor sequence
>5hlwA (length=284) Species: 9606 (Homo sapiens) [Search protein sequence]
ALNPELVQAVQHVVIGSSLIVHFNEVIGRHFGCVYHGTLLDGKKIHCAVK
SLNRIDIGEVSQFLTEGIIMKDFSHPNVLSLLGICSPLVVLPYMKHGDLR
NFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAARNCMLDEKF
TVKVADFGLARDMHDKEYYSVAKLPVKWMALESLQTQKFTTKSDVWSFGV
LLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCWH
PKAEMRPSFSELVSRISAIFSTFIGEHYVHVNAT
3D structure
PDB5hlw 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
[Spin on]
[Spin off]
[Reset orientation]

[High quality]
[Low quality]

[White background]
[Black background]

[Download]
[Download structure with residue number starting from 1]
Enzymatic activity
Catalytic site (original residue number in PDB) D1204 A1206 R1208 N1209 D1222 A1243
Catalytic site (residue number reindexed from 1) D138 A140 R142 N143 D156 A172
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 62E A I1084 A1108 Y1159 M1160 K1161 G1163 M1211 D1222 H1230 I27 A48 Y93 M94 K95 G97 M145 D156 H164 MOAD: ic50=23nM
PDBbind-CN: -logKd/Ki=7.64,IC50=23nM
BindingDB: IC50=29nM
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:5hlw, PDBe:5hlw, PDBj:5hlw
PDBsum5hlw
PubMed27355974
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

[Back to BioLiP]