Compound name
AMG PERK 44
Protein family
Protein Kinase
Target name
EIF2AK3
Affinity biochemical (nM)
6
Affinity on-target cellular (nM)
84
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002895aCl
SMILES
O=C1N(C2=CC=CC=C2)N(C)C(C3=CC=CC=C3)=C1C(C4=CC=C(C)C(C5=CC=C6N=C(C)C=CC6=C5)=C4N)=O.[H]Cl
InChIKey
YPPSMYLMSKHYAY-UHFFFAOYSA-N
NCBI gene ID
9451
UniProt ID
Q9NZJ5
Synonyms
PEK, PERK
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay (Cisbio Inc., using 1 µM ATP (=Km) )
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/25587754/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
ELISA (phosphorylation of PERK (T980) using HT1080–T-REx–PERK–FLAG cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/25587754/
Affinity on-target cellular relation
=
Selectivity platform
KINOMEscan (DiscoveRx)
Selectivity platform number of targets
387
Selectivity remarks
Screened at 1 µM, closest targets as % of control: CSF1R (40%), NEK11 (41%), full screening data available as supporting information, https://pubmed.ncbi.nlm.nih.gov/25587754/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/25587754/
Selectivity Number of Off-targets
0