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Target
Interferon-induced, double-stranded RNA-activated protein kinase
Ligand
BDBM50308060
Substrate
n/a
Meas. Tech.
ChEMBL_655901 (CHEMBL1244945)
Kd
120±n/a nM
Citation
 Zarrinkar, PP; Gunawardane, RN; Cramer, MD; Gardner, MF; Brigham, D; Belli, B; Karaman, MW; Pratz, KW; Pallares, G; Chao, Q; Sprankle, KG; Patel, HK; Levis, M; Armstrong, RC; James, J; Bhagwat, SS AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 114:2984-92 (2009) [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:
BDBM50308060
Synonyms:
16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8(13),9,11,20(25),21,23-nonaen-3-one | CEP-701 | CHEMBL603469 | US11370779, Compound CEP-701
Type:
Small organic molecule
Emp. Form.:
C26H21N3O4
Mol. Mass.:
439.4626
SMILES:
C[C@]12O[C@H](C[C@]1(O)CO)n1c3ccccc3c3c4C(=O)NCc4c4c5ccccc5n2c4c13 |r|
Structure:
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