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Target
Interferon-induced, double-stranded RNA-activated protein kinase
Ligand
BDBM50442163
Substrate
n/a
Meas. Tech.
ChEMBL_993289 (CHEMBL2443946)
IC50
99±n/a nM
Citation
 Axten, JM; Romeril, SP; Shu, A; Ralph, J; Medina, JR; Feng, Y; Li, WH; Grant, SW; Heerding, DA; Minthorn, E; Mencken, T; Gaul, N; Goetz, A; Stanley, T; Hassell, AM; Gampe, RT; Atkins, C; Kumar, R Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development. ACS Med Chem Lett 4:964-8 (2013) [PubMed]  Article 
Target
Name:
Interferon-induced, double-stranded RNA-activated protein kinase
Synonyms:
E2AK2_HUMAN | EIF2AK2 | Eukaryotic translation initiation factor 2-alpha kinase 2 | Interferon-inducible RNA-dependent protein kinase | P1/eIF-2A protein kinase | PKR | PRKR | Protein kinase R | Protein kinase RNA-activated | Tyrosine-protein kinase EIF2AK2 | eIF-2A protein kinase 2 | p68 kinase
Type:
PROTEIN
Mol. Mass.:
62104.61
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1467743
Residue:
551
Sequence:
MAGDLSAGFFMEELNTYRQKQGVVLKYQELPNSGPPHDRRFTFQVIIDGREFPEGEGRSKKEAKNAAAKLAVEILNKEKKAVSPLLLTTTNSSEGLSMGNYIGLINRIAQKKRLTVNYEQCASGVHGPEGFHYKCKMGQKEYSIGTGSTKQEAKQLAAKLAYLQILSEETSVKSDYLSSGSFATTCESQSNSLVTSTLASESSSEGDFSADTSEINSNSDSLNSSSLLMNGLRNNQRKAKRSLAPRFDLPDMKETKYTVDKRFGMDFKEIELIGSGGFGQVFKAKHRIDGKTYVIKRVKYNNEKAEREVKALAKLDHVNIVHYNGCWDGFDYDPETSDDSLESSDYDPENSKNSSRSKTKCLFIQMEFCDKGTLEQWIEKRRGEKLDKVLALELFEQITKGVDYIHSKKLIHRDLKPSNIFLVDTKQVKIGDFGLVTSLKNDGKRTRSKGTLRYMSPEQISSQDYGKEVDLYALGLILAELLHVCDTAFETSKFFTDLRDGIISDIFDKKEKTLLQKLLSKKPEDRPNTSEILRTLTVWKKSPEKNERHTC
  
Inhibitor
Name:
BDBM50442163
Synonyms:
CHEMBL2441346
Type:
Small organic molecule
Emp. Form.:
C22H22FN7O
Mol. Mass.:
419.4548
SMILES:
Cc1cc(C)n(CC(=O)N2CCc3c2ccc(-c2cn(C)c4ncnc(N)c24)c3F)n1
Structure:
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