Compile Data Set for Download or QSAR
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Found 6 Enz. Inhib. hit(s) for PDB: 4X7N
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072036(CHEMBL3407862)
Affinity DataIC50:  6nMAssay Description:Inhibition of human N-terminal His-tagged PERK expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s...More data for this Ligand-Target Pair
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072036(CHEMBL3407862)
Affinity DataIC50:  84nMAssay Description:Inhibition of doxycycline-inducible T-REx-PERK-FLAG (unknown origin) autophosphorylation tranfected in human HT1080 cells after 1 hr by sandwich ELIS...More data for this Ligand-Target Pair
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072036(CHEMBL3407862)
Affinity DataIC50:  770nMAssay Description:Inhibition of PERK in human HT1080 cells assessed as inhibition of thapsigargin-induced CHoP mRNA expression preincubated for 1 hr followed by thapsi...More data for this Ligand-Target Pair
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072036(CHEMBL3407862)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of GCN2 in amino acid starved human HT1080 cells assessed as inhibition of CHoP mRNA expression preincubated for 1 hr followed by 2 hrs in...More data for this Ligand-Target Pair
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072036(CHEMBL3407862)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of GCN2 phosphorylation in human U2OS cells preincubated for 1 hr followed by drug wash out and incubated for 2 hrs by MSD assayMore data for this Ligand-Target Pair
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072036(CHEMBL3407862)
Affinity DataEC50:  400nMAssay Description:Inhibition of PERK-mediated protein synthesis in human U2OS cells harboring thapsigargin-induced ER stress assessed as incorporation of L-azidohomoal...More data for this Ligand-Target Pair