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TargetInterferon-induced, double-stranded RNA-activated protein kinase
LigandBDBM50396531
Substrate/Competitorn/a
Meas. Tech.ChEMBL_862849 (CHEMBL2172951)
IC50 978±n/a nM
Citation Axten, JMMedina, JRFeng, YShu, ARomeril, SPGrant, SWLi, WHHeerding, DAMinthorn, EMencken, TAtkins, CLiu, QRabindran, SKumar, RHong, XGoetz, AStanley, TTaylor, JDSigethy, SDTomberlin, GHHassell, AMKahler, KMShewchuk, LMGampe, RT 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). J Med Chem55:7193-207 (2012) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Interferon-induced, double-stranded RNA-activated protein kinase
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:
MAGDLSAGFFMEELNTYRQKQGVVLKYQELPNSGPPHDRRFTFQVIIDGREFPEGEGRSK
KEAKNAAAKLAVEILNKEKKAVSPLLLTTTNSSEGLSMGNYIGLINRIAQKKRLTVNYEQ
CASGVHGPEGFHYKCKMGQKEYSIGTGSTKQEAKQLAAKLAYLQILSEETSVKSDYLSSG
SFATTCESQSNSLVTSTLASESSSEGDFSADTSEINSNSDSLNSSSLLMNGLRNNQRKAK
RSLAPRFDLPDMKETKYTVDKRFGMDFKEIELIGSGGFGQVFKAKHRIDGKTYVIKRVKY
NNEKAEREVKALAKLDHVNIVHYNGCWDGFDYDPETSDDSLESSDYDPENSKNSSRSKTK
CLFIQMEFCDKGTLEQWIEKRRGEKLDKVLALELFEQITKGVDYIHSKKLIHRDLKPSNI
FLVDTKQVKIGDFGLVTSLKNDGKRTRSKGTLRYMSPEQISSQDYGKEVDLYALGLILAE
LLHVCDTAFETSKFFTDLRDGIISDIFDKKEKTLLQKLLSKKPEDRPNTSEILRTLTVWK
KSPEKNERHTC
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BDBM50396531
n/a
NameBDBM50396531
Synonyms:CHEMBL2171132
TypeSmall organic molecule
Emp. Form.C27H23N5OS
Mol. Mass.465.569
SMILESCn1cc(cn1)-c1cnc(N)c2c(csc12)-c1ccc2N(CCc2c1)C(=O)Cc1ccccc1
Structure
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