Structure of PDB 5tr6 Chain A

Receptor sequence
>5tr6A (length=272) Species: 9606 (Homo sapiens) [Search protein sequence]
EVYLDRKLLTLEDKELGSGNFGTVKKGYYQMKKVVKTVAVKILPALKDEL
LAEANVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQQNRHVK
DKNIIELVHQVSMGMKYLEESNFVHRDLAARNVLLVTQHYAKISDFGLSK
ALRADENYYKAQTHGKWPVKWYAPECINYYKFSSKSDVWSFGVLMWEAFS
YGQKPYRGMKGSEVTAMLEKGERMGCPAGCPREMYDLMNLCWTYDVENRP
GFAAVELRLRNYYYDVVNHHHH
3D structure
PDB5tr6 Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).
ChainA
Resolution1.93 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D494 A496 R498 N499 D512 K533
Catalytic site (residue number reindexed from 1) D127 A129 R131 N132 D145 K166
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 7KG A A400 E449 M450 A451 G454 P455 R498 L501 S511 D512 A39 E82 M83 A84 G87 P88 R131 L134 S144 D145 MOAD: ic50=3.2nM
PDBbind-CN: -logKd/Ki=8.49,IC50=3.2nM
BindingDB: IC50=2.0nM,EC50=9.8nM
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:5tr6, PDBe:5tr6, PDBj:5tr6
PDBsum5tr6
PubMed27839918
UniProtP43405|KSYK_HUMAN Tyrosine-protein kinase SYK (Gene Name=SYK)

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