Compound name
PF-06260933
Protein family
Protein Kinase
Target name
MAP4K4
Affinity biochemical (nM)
3.7
Affinity on-target cellular (nM)
160
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001888a
SMILES
NC1=C(C2=CC=C(Cl)C=C2)C=C(C(C=N3)=CC=C3N)C=N1
InChIKey
KHPCIHZXOGHCLY-UHFFFAOYSA-N
NCBI gene ID
9448
UniProt ID
O95819
Synonyms
HGK, NIK, FLH21957
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
FRET assay (conc. ATP = 10 µM)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/26617966/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
ELISA (inhibition of MAP4K4’s phosphorylation of serine/threonine residues on traf2, using Cell Maintenance GripTite™ 293 MSR Cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/26617966/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (ActivX assay using human peripheral blood monomuclear cells, PBMC)
Selectivity platform number of targets
150
Selectivity remarks
Screened at 1 µM and 10 µM, the closest targets as % of inhibition at 1 µM: GCK (52.7%), PIP4K2C (53.1%), HGK (83%), TNIK (97.2%), full screening data are available as supporting information,file:///C:/Users/roehm.admin/Downloads/ml5b00215_si_001.pdf;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/26617966/
Selectivity Number of Off-targets
0