Structure of PDB 5cy3 Chain A

Receptor sequence
>5cy3A (length=276) Species: 9606 (Homo sapiens) [Search protein sequence]
PKEVYLDRKLLTLEDKELGSGNFGTVKKGYYQMKKVVKTVAVKILKNEDP
ALKDELLAEANVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQ
QNRHVTDKNIIELVHQVSMGMKYLEESNFVHRDLAARNVLLVTQHYAKIS
DFGLSKALRADENYYKAQTHGKWPVKWYAPECINYYKFSSKSDVWSFGVL
MWEAFSYGQKPYRGMKGSEVTAMLEKGERMGCPAGCPREMYDLMNLCWTY
DVENRPGFAAVELRLRNYYYDVVNEG
3D structure
PDB5cy3 Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
ChainA
Resolution1.76 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) D133 A135 R137 N138 D151 K172
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 55Y A L377 V385 A400 K402 M448 A451 G454 L501 S511 D512 L18 V26 A41 K43 M87 A90 G93 L140 S150 D151 MOAD: ic50=16nM
PDBbind-CN: -logKd/Ki=7.80,IC50=16nM
BindingDB: IC50=16nM
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:5cy3, PDBe:5cy3, PDBj:5cy3
PDBsum5cy3
PubMed26320624
UniProtP43405|KSYK_HUMAN Tyrosine-protein kinase SYK (Gene Name=SYK)

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