Structure of PDB 5cxz Chain A

Receptor sequence
>5cxzA (length=269) Species: 9606 (Homo sapiens) [Search protein sequence]
VYLDRKLLTLEDKELGSGNFGTVKKGYYQMKKVVKTVAVKILKNALKDEL
LAEANVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQQNRHVT
DKNIIELVHQVSMGMKYLEESNFVHRDLAARNVLLVTQHYAKISDFGLSK
ALRADENYYKAQTHKWPVKWYAPECINYYKFSSKSDVWSFGVLMWEAFSY
GQKPYRGMKGSEVTAMLEKGERMGCPAGCPREMYDLMNLCWTYDVENRPG
FAAVELRLRNYYYDVVNHH
3D structure
PDB5cxz Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
ChainA
Resolution1.7 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 K165
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 55U A L377 A400 M450 A451 G454 P455 L501 D512 L15 A38 M83 A84 G87 P88 L134 D145 MOAD: ic50=552nM
PDBbind-CN: -logKd/Ki=6.26,IC50=552nM
BindingDB: IC50=34nM
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:5cxz, PDBe:5cxz, PDBj:5cxz
PDBsum5cxz
PubMed26320624
UniProtP43405|KSYK_HUMAN Tyrosine-protein kinase SYK (Gene Name=SYK)

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