Compound name
eFT508
Protein family
Protein Kinase
Target name
MKNK2
Affinity biochemical (nM)
1
Affinity on-target cellular (nM)
1
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0002081a
SMILES
NC1=NC=NC(NC2=CC(C)=C(C(NC34CCCCC4)=O)N3C2=O)=C1
InChIKey
HKTBYUWLRDZAJK-UHFFFAOYSA-N
NCBI gene ID
2872
UniProt ID
Q9HBH9
Synonyms
MNK2
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
ADP-Glo kinase assay (Promega, using 10 µM ATP)
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01795#
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot assay (inhibition of eIF4E phosphorylation at Ser209 using HEK293 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/30530193/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (literature)
Selectivity platform number of targets
419
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition: MKNK1 (104%), MKNK2 (93%), STK17A (82%), CLK4 (60%), full screening data available as supplemental information, https://pubs.acs.org/doi/suppl/10.1021/acs.jmedchem.7b01795/suppl_file/jm7b01795_si_002.pdf;
In-vitro potency (enzymatic assay): IC50(MKNK1) = 2 nM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01795#;
In-vitro potency (enzymatic assay): IC50(MKNK2) = 1 nM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01795#;
In-vitro potency (enzymatic assay): IC50(STK17A) = 130 nM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01795#;
In-vitro potency (enzymatic assay): IC50(CLK4) = 790 nM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01795#;
In-vitro potency (enzymatic assay): IC50(MKNK1) = 2 nM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01795#;
In-vitro potency (enzymatic assay): IC50(MKNK2) = 1 nM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01795#;
In-vitro potency (enzymatic assay): IC50(STK17A) = 130 nM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01795#;
In-vitro potency (enzymatic assay): IC50(CLK4) = 790 nM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01795#;
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01795#
Selectivity Number of Off-targets
2