Structure of PDB 2og8 Chain A

Receptor sequence
>2og8A (length=246) Species: 9606 (Homo sapiens) [Search protein sequence]
EWEVPRETLKLVERLGAGQFGEVWMGYYNGHTKVAVKSLKQGSMSPDAFL
AEANLMKQLQHQRLVRLYAVVTQEPIYIITEYMENGSLVDFLKTPSGIKL
TINKLLDMAAQIAEGMAFIEERNYIHRDLRAANILVSDTLSCKIADFGLP
IKWTAPEAINYGTFTIKSDVWSFGILLTEIVTHGRIPYPGMTNPEVIQNL
ERGYRMVRPDNCPEELYQLMRLCWKERPEDRPTFDYLRSVLEDFFT
3D structure
PDB2og8 Discovery of Aminoquinazolines as Potent, Orally Bioavailable Inhibitors of Lck: Synthesis, SAR, and in Vivo Anti-Inflammatory Activity
ChainA
Resolution2.3 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D364 R366 A368 N369 D382
Catalytic site (residue number reindexed from 1) D128 R130 A132 N133 D146
Enzyme Commision number 2.7.10.2: non-specific 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 1N8 A A271 K273 E288 M292 L300 T316 Y318 M319 L371 A381 D382 F383 A35 K37 E52 M56 L64 T80 Y82 M83 L135 A145 D146 F147 MOAD: ic50=0.5nM
PDBbind-CN: -logKd/Ki=9.30,IC50=0.5nM
BindingDB: IC50=0.500000nM
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:2og8, PDBe:2og8, PDBj:2og8
PDBsum2og8
PubMed16970394
UniProtP06239|LCK_HUMAN Tyrosine-protein kinase Lck (Gene Name=LCK)

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