Compound name
GSK2606414
Protein family
Protein Kinase
Target name
EIF2AK3
Affinity biochemical (nM)
0.4
Affinity on-target cellular (nM)
3
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001324a
SMILES
Cn1cc(-c2ccc3c(c2)CCN3C(=O)Cc2cccc(C(F)(F)F)c2)c2c(N)ncnc21
InChIKey
SIXVRXARNAVBTC-UHFFFAOYSA-N
NCBI gene ID
9451
UniProt ID
Q9NZJ5
Synonyms
PEK, PERK
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
HTRF assay (cytoplasmic PERK domain phosphorylation of EIF2α)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/22827572/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot assay (inhibition of PERK autophosphorylation in A459 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/22827572/
Affinity on-target cellular relation
<
Selectivity platform
Kinase panel (Reaction Biology)
Selectivity platform number of targets
294
Selectivity remarks
Screened at 10 µM, using conc. ATP = Km, closest targets as % of control: DDR2 (0.08%), MAP3K9 (1.20%), MAP4K5 (3.22%), BRK (4.25%), MER(4.34%), MAP3K11 (4.40%), MYLK2 (4.41%), RET (4.80%), MAP3K10 (5.86%), NTRK1 (5.92%), NTRK3 (6.85%), IKBKE (8.81%), LCK (10.19%), full screening data available as supporting information, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro follow-up of closest targets in the screen (enzymatic assay, ReactionBiology): IC50(KIT) = 154 nM, IC50(AURKB) = 407 nM, IC50(BRK) = 412 nM, IC50(MAP3K10) = 452 nM, IC50(MER) = 474 nM, IC50(DDR2) = 524 nM, IC50(MYLK2) = 701 nM, IC50(IKBKE) = 1064 nM, IC50(MAP3K11) = 1140 nM, IC500(RET) = 1215 nM, IC50(LCK) = 1250 nM, IC50(NEK4) = 1402 nM, IC50(MAP4K5) = 1569 nM, IC50(MAp3K9) = 1578 nM, IC50(NTRK1) = 1756 nM, IC50(AXL) = 2705 nM, IC50(YES1) = 3195 nM, IC50(WNK2) = 3892 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (HTRF assay): IC50(EIF2AK1) = 420 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (HTRF assay): IC50(EIF2AK2) = 696 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (ADP-Glo assay): IC50(RIPK1) = 18.2 nM, https://www.nature.com/articles/cdd201758;
In-vitro follow-up of closest targets in the screen (enzymatic assay, ReactionBiology): IC50(KIT) = 154 nM, IC50(AURKB) = 407 nM, IC50(BRK) = 412 nM, IC50(MAP3K10) = 452 nM, IC50(MER) = 474 nM, IC50(DDR2) = 524 nM, IC50(MYLK2) = 701 nM, IC50(IKBKE) = 1064 nM, IC50(MAP3K11) = 1140 nM, IC500(RET) = 1215 nM, IC50(LCK) = 1250 nM, IC50(NEK4) = 1402 nM, IC50(MAP4K5) = 1569 nM, IC50(MAp3K9) = 1578 nM, IC50(NTRK1) = 1756 nM, IC50(AXL) = 2705 nM, IC50(YES1) = 3195 nM, IC50(WNK2) = 3892 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (HTRF assay): IC50(EIF2AK1) = 420 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (HTRF assay): IC50(EIF2AK2) = 696 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (ADP-Glo assay): IC50(RIPK1) = 18.2 nM, https://www.nature.com/articles/cdd201758;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/22827572/
Selectivity Number of Off-targets
7