Compound name
GCN2iB
Protein family
Protein Kinase
Target name
EIF2AK4
Affinity biochemical (nM)
2.4
Affinity on-target cellular (nM)
80
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002919a
SMILES
O=S(C1=CC(Cl)=CN=C1OC)(NC2=CC=C(F)C(C#CC3=CN=C(N)N=C3)=C2F)=O
InChIKey
JGHVXJKGYJYWOP-UHFFFAOYSA-N
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Lantha Screen assay (LanthaScreen Tb-anti-p-eIF2α (pSer52) antibody kit (Thermo Fisher Scientific) using ATP = Km)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/30061420/
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Western Blot assay (phosphorylation of GCN2 using CCRF-CEM cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/30061420/
Affinity on-target cellular relation
>
Selectivity platform
KINOMEscan (DiscoveRx)
Selectivity platform number of targets
468
Selectivity remarks
Screened at 1 µM, closest targets >95 % of control: MAP2K5, STK10, ZAK, GSK3B (100%) further targets not named;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/30061420/
Selectivity Number of Off-targets
3