Structure of PDB 5lmb Chain A

Receptor sequence
>5lmbA (length=265) Species: 9606 (Homo sapiens) [Search protein sequence]
YLDRKLLTLEDKELGSGNFGTVKKGYYQMKKVVKTVAVKILPALKDELLA
EANVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQQNRHVKDK
NIIELVHQVSMGMKYLEESNFVHRDLAARNVLLVTQHYAKISDFGLSKAL
RADENYYKAQTHGKWPVKWYAPECINYYKFSSKSDVWSFGVLMWEAFSYG
QKPYRGMKGSEVTAMLEKGERMGCPAGCPREMYDLMNLCWTYDVENRPGF
AAVELRLRNYYYDVV
3D structure
PDB5lmb Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors.
ChainA
Resolution1.95 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 6ZF A L377 A400 M450 A451 G454 P455 R498 N499 L501 D512 L14 A37 M81 A82 G85 P86 R129 N130 L132 D143 MOAD: ic50=16nM
PDBbind-CN: -logKd/Ki=7.80,IC50=15.8nM
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:5lmb, PDBe:5lmb, PDBj:5lmb
PDBsum5lmb
PubMed27578246
UniProtP43405|KSYK_HUMAN Tyrosine-protein kinase SYK (Gene Name=SYK)

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