Compound name
GSK2656157
Protein family
Protein Kinase
Target name
EIF2AK3
Affinity biochemical (nM)
0.9
Affinity on-target cellular (nM)
10
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001237a
SMILES
Cc1cccc(CC(=O)N2CCc3c2ccc(-c2cn(C)c4ncnc(N)c24)c3F)n1
InChIKey
PRWSIEBRGXYXAJ-UHFFFAOYSA-N
NCBI gene ID
9451
UniProt ID
Q9NZJ5
Synonyms
PEK, PERK
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23333938/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot assay (inhibition of PERK downstream substrate, phospho-eIF2α, in BxPC3 pancreatic tumor cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/23333938/
Affinity on-target cellular relation
<
Selectivity platform
Kinase panel (Reaction Biology)
Selectivity platform number of targets
300
Selectivity remarks
Screened at 10 µM (using 10 µM ATP), closest targets as % of inhibition: NEK1 (96.76%), MAP4K5(96.28%), MEKK2(94.29%), MER(92.85%), MAP3K10(9.2%), RPS6KA5(86.83%), full screening data are available as supporting information; In-vitro potency of closest targets (enzymatic assay): IC50(EIF2AK1) = 460 nM, IC50(BRK) = 822 nM, IC50(EIF2AK2) = 905 nM, IC50(MEKK2) = 954 nM, IC50(NEK1) = 9807 nM, IC50(MAP4K5) = 1764 nM, IC50(MEKK3) = 2847 nM, IC50(MER) = 3431 nM, IC50(MAP3K10) = 2796 nM, full screening data available in manuscript, https://pubmed.ncbi.nlm.nih.gov/23333938/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23333938/
Selectivity Number of Off-targets
5