Reaction Details |
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Target | Interferon-induced, double-stranded RNA-activated protein kinase |
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Ligand | BDBM50396531 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_862849 (CHEMBL2172951) |
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IC50 | 978±n/a nM |
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Citation | Axten, JM; Medina, JR; Feng, Y; Shu, A; Romeril, SP; Grant, SW; Li, WH; Heerding, DA; Minthorn, E; Mencken, T; Atkins, C; Liu, Q; Rabindran, S; Kumar, R; Hong, X; Goetz, A; Stanley, T; Taylor, JD; Sigethy, SD; Tomberlin, GH; Hassell, AM; Kahler, KM; Shewchuk, LM; Gampe, 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 |
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More Info.: | Get all data from this article, Assay Method |
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Interferon-induced, double-stranded RNA-activated protein kinase |
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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 |
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n/a |
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Name | BDBM50396531 |
Synonyms: | CHEMBL2171132 |
Type | Small organic molecule |
Emp. Form. | C27H23N5OS |
Mol. Mass. | 465.569 |
SMILES | Cn1cc(cn1)-c1cnc(N)c2c(csc12)-c1ccc2N(CCc2c1)C(=O)Cc1ccccc1 |
Structure |
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