Compound name
DLK-IN-1
Protein family
Protein Kinase
Target name
MAP3K12
Affinity biochemical (nM)
3
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001895a
SMILES
CC(N1C([C@@H]2[C@]3([H])[C@@]2([H])CN(C4COC4)C3)=CC(C5=CN=C(N)C(OC(F)(F)F)=C5)=N1)C
InChIKey
UHEFRVBGJORHNV-UOIKSKOESA-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/28929759/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (Life Technologies Kinase Assays)
Selectivity platform number of targets
220
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition, FLT3 (52.2%), PAK4 (69.5%), NTRK1 (67.1%), full screening data available in paper; In-vitro potency (TR-FRET assay): IC50(FLT3) = 709 nM, IC50(PAK4) = 673 nM, IC50(STK16) = 1520 nM, IC50(NTRK1) = 1500 nM, https://pubmed.ncbi.nlm.nih.gov/28929759/;
Screened at 10 µM, against 42 targets (biogenic amine receptors, neuropeptide receptors, ion channels, and neurotransmitter transporters), CEREP Receptor panel, closest targets as % of control: A2A (18%), D2s (19%), PPARd (12%), full screening data available as supporting information, https://pubmed.ncbi.nlm.nih.gov/28929759/;
Screened at 10 µM, against 42 targets (biogenic amine receptors, neuropeptide receptors, ion channels, and neurotransmitter transporters), CEREP Receptor panel, closest targets as % of control: A2A (18%), D2s (19%), PPARd (12%), full screening data available as supporting information, https://pubmed.ncbi.nlm.nih.gov/28929759/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/28929759/
Selectivity Number of Off-targets
2