Structure of PDB 4g34 Chain A

Receptor sequence
>4g34A (length=248) Species: 9606 (Homo sapiens) [Search protein sequence]
GRYLTDFEPIQCLGRGGFGVVFEAKNKVDDCNYAIKRIRLPNRELAREKV
MREVKALAKLEHPGIVRYFNAWLEKNKVYLYIQMQLCRKENLKDWMNGRC
TIEERERSVCLHIFLQIAEAVEFLHSKGLMHRDLKPSNIFFTMDDVVKVG
DFGLGTKLYMSPEQIHGNSYSHKVDIFSLGLILFELLYPFSTQMERVRTL
TDVRNLKFPPLFTQKYPCEYVMVQDMLSPSPMERPEAINIIENAVFED
3D structure
PDB4g34 Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK).
ChainA
Resolution2.7 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D936 K938 N941 D954 T986
Catalytic site (residue number reindexed from 1) D133 K135 N138 D151 T156
Enzyme Commision number 2.7.11.1: non-specific serine/threonine protein 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 924 A A619 L642 Y653 M887 C890 D954 A34 L57 Y68 M84 C87 D151 PDBbind-CN: -logKd/Ki=7.93,IC50=11.7nM
BindingDB: IC50=>300nM
Gene Ontology
Molecular Function
GO:0004672 protein 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:4g34, PDBe:4g34, PDBj:4g34
PDBsum4g34
PubMed22827572
UniProtQ9NZJ5|E2AK3_HUMAN Eukaryotic translation initiation factor 2-alpha kinase 3 (Gene Name=EIF2AK3)

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