Structure of PDB 4i0r Chain A

Receptor sequence
>4i0rA (length=264) Species: 9606 (Homo sapiens) [Search protein sequence]
VYLDRKLLTLEDELGSGTVKKGYYQMKKVVKTVAVKILKPALKDELLAEA
NVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQQNRHVKDKNI
IELVHQVSMGMKYLEESNFVHRDLAARNVLLVTQHYAKISDFGLSKALRA
DENYYKAKWPVKWYAPECINYYKFSSKSDVWSFGVLMWEAFSYGQKPYRG
MKGSEVTAMLEKGERMGCPAGCPREMYDLMNLCWTYDVENRPGFAAVELR
LRNYYYDVVNEGHH
3D structure
PDB4i0r Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.
ChainA
Resolution2.1 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) D123 A125 R127 N128 D141 K158
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 1B4 A A400 M448 M450 A451 E452 G454 P455 L501 A34 M77 M79 A80 E81 G83 P84 L130 MOAD: ic50=14nM
PDBbind-CN: -logKd/Ki=7.85,IC50=14nM
BindingDB: IC50=190nM
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:4i0r, PDBe:4i0r, PDBj:4i0r
PDBsum4i0r
PubMed23350847
UniProtP43405|KSYK_HUMAN Tyrosine-protein kinase SYK (Gene Name=SYK)

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