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Target
Interferon-induced, double-stranded RNA-activated protein kinase
Ligand
BDBM25118
Substrate
n/a
Meas. Tech.
ChEMBL_586721 (CHEMBL1062867)
Kd
2800±n/a nM
Citation
Karaman, MW; Herrgard, S; Treiber, DK; Gallant, P; Atteridge, CE; Campbell, BT; Chan, KW; Ciceri, P; Davis, MI; Edeen, PT; Faraoni, R; Floyd, M; Hunt, JP; Lockhart, DJ; Milanov, ZV; Morrison, MJ; Pallares, G; Patel, HK; Pritchard, S; Wodicka, LM; Zarrinkar, PP A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol 26:127-32 (2008) [PubMed] Article
More Info.:
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:
BDBM25118
Synonyms:
(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril | 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-1,3-benzodiazol-2-yl]-1,2-dihydroquinolin-2-one | CHEMBL522892 | CHIR-258
Type:
Small organic molecule
Emp. Form.:
C21H21FN6O
Mol. Mass.:
392.4294
SMILES:
CN1CCN(CC1)c1ccc2nc([nH]c2c1)-c1c(N)c2c(F)cccc2[nH]c1=O