Structure of PDB 6n3o Chain A

Receptor sequence
>6n3oA (length=252) Species: 9606 (Homo sapiens) [Search protein sequence]
SRYFIEFEELQLLGKGAFGAVIKVQNKLDGCCYAVKRIPINPASRQFRRI
KGEVTLLSRLHHENIVRYYNAWIENAVHYLYIQMEYCEASTLRDTIDQGL
YRDTVRLWRLFREILDGLAYIHEKGMIHRNLKPVNIFLDSDDHVKIGDFG
LATDHLAFSEALYVSPEYNQKVDLFSLGIIFFEMSYHPMVTASERIFVLN
QLRDPTSPKFPEDFDDGEHAKQKSVISWLLNHDPAKRPTATELLKSELLP
PP
3D structure
PDB6n3o Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.
ChainA
Resolution2.4 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) N848 K850 N853 D866 E904
Catalytic site (residue number reindexed from 1) N130 K132 N135 D148 E160
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 KA7 A L596 A617 K619 L640 Y651 M802 Y804 C805 F855 D866 F867 L13 A34 K36 L57 Y68 M84 Y86 C87 F137 D148 F149 MOAD: ic50=2.4nM
PDBbind-CN: -logKd/Ki=8.62,IC50=2.4nM
Gene Ontology
Molecular Function
GO:0004672 protein 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:6n3o, PDBe:6n3o, PDBj:6n3o
PDBsum6n3o
PubMed31620240
UniProtQ9P2K8|E2AK4_HUMAN eIF-2-alpha kinase GCN2 (Gene Name=EIF2AK4)

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