Compound name
GNE-3511
Protein family
Protein Kinase
Target name
MAP3K12
Affinity biochemical (nM)
8
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0002063a
SMILES
FC(C1)(F)CCN1C2=CC(C3CCN(C4COC4)CC3)=CC(NC5=CC(C#N)=CC=N5)=N2
InChIKey
RHFIAUKMKYHHFA-UHFFFAOYSA-N
NCBI gene ID
7786
UniProt ID
Q12852
Synonyms
MUK, DLK, ZPKP1, MEKK12
Mode of action
Inhibitor
Affinity biochemical definition
Ki
Affinity biochemical assay type
Enzymatic assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/25341110/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (Invitrogen)
Selectivity platform number of targets
298
Selectivity remarks
Screened at 100 nM, in-vitro potency of closest targets (enzymatic assay, Invitrogen): Ki(MAP3K12) <0.5 nM, IC50(MAP2K4) >5000 nM, IC50(MAP2K7) >5000 nM, IC50(MAPK8) = 129 nM, IC50(MAPK9) = 514 nM, IC50(MAPK10) = 364 nM, IC50(MLK1) = 67.8 nM, IC50(MLK2) = 767 nM, IC50(MLK3) = 602 nM, https://pubmed.ncbi.nlm.nih.gov/25341110/;
Selectivity Number of Off-targets
6