Structure of PDB 4pv0 Chain A

Receptor sequence
>4pv0A (length=268) Species: 9606 (Homo sapiens) [Search protein sequence]
VYLDRKLLTLEDKELGSFGTVKKGYYQMKKVVKTVAVKILKPALKDELLA
EANVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQQNRHVKDK
NIIELVHQVSMGMKYLEESNFVHRDLAARNVLLVTQHYAKISDFGLSKAL
RADENYYKAQTHGKWPVKWYAPECINYYKFSSKSDVWSFGVLMWEAFSYG
QKPYRGMKGSEVTAMLEKGERMGCPAGCPREMYDLMNLCWTYDVENRPGF
AAVELRLRNYYYDVVNEG
3D structure
PDB4pv0 Discovery of GS-9973, a Selective and Orally Efficacious Inhibitor of Spleen Tyrosine Kinase.
ChainA
Resolution2.0 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) D125 A127 R129 N130 D143 K164
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 CG4 A V385 A400 A451 E452 G454 P455 K458 L501 V21 A36 A82 E83 G85 P86 K89 L132 MOAD: Kd=4nM
PDBbind-CN: -logKd/Ki=9.07,IC50=0.85nM
BindingDB: IC50=0.840000nM,EC50=175nM,Kd=4.0nM
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:4pv0, PDBe:4pv0, PDBj:4pv0
PDBsum4pv0
PubMed24779514
UniProtP43405|KSYK_HUMAN Tyrosine-protein kinase SYK (Gene Name=SYK)

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