Compound name
GNE-8505
Protein family
Protein Kinase
Target name
MAP3K12
Affinity biochemical (nM)
10
Affinity on-target cellular (nM)
77.6
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002923a
SMILES
FC(F)(F)C1=CC(C2=NN(C([C@@H]3[C@]4([H])[C@@]3([H])CN(C5COC5)C4)=C2)CC6CC6)=CN=C1N
InChIKey
IRPVABHDSJVBNZ-QWHZDKJVSA-N
NCBI gene ID
7786
UniProt ID
Q12852
Synonyms
MUK, DLK, ZPKP1, MEKK12
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.2c01056
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Immunoblot assay (JNK phosphorylation in HEK293 cells overexpressing DLK, calculated serum-free assay)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/28814543/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (invitrogen)
Selectivity platform number of targets
220
Selectivity remarks
Screened at 1 µM, closest targets as % of control: FLT3 (67%), DMPK (58%), AXL (57%), NTRK1 (56%), CSF1R (54%), EPHA7 (51%), further screening data not shown in paper, https://pubmed.ncbi.nlm.nih.gov/28814543/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/28814543/
Selectivity Number of Off-targets
0