BDBM50072035 CHEMBL3407861

SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(sc2c1)C(F)(F)F

InChI Key InChIKey=DRQQNHJHIDNZOM-UHFFFAOYSA-N

Data  7 IC50  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 8 hits for monomerid = 50072035   

TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072035(CHEMBL3407861)
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
In DepthDetails ArticlePubMed
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072035(CHEMBL3407861)
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
In DepthDetails ArticlePubMed
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072035(CHEMBL3407861)
Affinity DataIC50:  53nMAssay 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
In DepthDetails ArticlePubMed
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072035(CHEMBL3407861)
Affinity DataIC50:  3.00E+3nMAssay 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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072035(CHEMBL3407861)
Affinity DataIC50: >1.00E+3nMAssay Description:Inhibition of recombinant BRAF V600E kinase domain mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072035(CHEMBL3407861)
Affinity DataIC50:  88nMAssay 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
In DepthDetails ArticlePubMed
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072035(CHEMBL3407861)
Affinity DataEC50:  1.30E+3nMAssay 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
In DepthDetails ArticlePubMed
TargeteIF-2-alpha kinase GCN2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50072035(CHEMBL3407861)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of human C-terminal His-tagged GCN2 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
In DepthDetails ArticlePubMed