Compound name
BAY-8400
Protein family
Protein Kinase
Target name
PRKDC
Affinity biochemical (nM)
81
Affinity on-target cellular (nM)
69
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001679b
SMILES
FC(C1=CC(C2=CC=C3N=CC4=NN=C(N4C3=C2)C5=CCCOCC5)=CN=C1)F
InChIKey
ATKHYZXUMVNCIO-UHFFFAOYSA-N
NCBI gene ID
5591
UniProt ID
P78527
Synonyms
DNPK1, p350, DNAPK, XRCC7, DNA-PKcs, DNAPKc, DNA-PKC, p460
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET (using 2 mM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/34428039/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Immunoblot assay (PRKDC dependent inhibition of histone H2AX -Ser139 phosphorylation (G-H2AX) in HT-144 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/34428039/
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
365
Selectivity remarks
Screened at 1 µM, closest targets as % of control: PRKDC (-1%), PIK3C2G (-12%), MTOR (41%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/34428039/;
In-cellular potency (Immunoblot assay, ATR dependent inhibition of histone H2AX -Ser139 phosphorylation (G-H2AX) in HT-144 cells): IC50(ATR) = 2360 nM, https://pubmed.ncbi.nlm.nih.gov/34428039/;
In-cellular potency (Immunoblot assay, ATR dependent inhibition of histone H2AX -Ser139 phosphorylation (G-H2AX) in HT-144 cells): IC50(ATR) = 2360 nM, https://pubmed.ncbi.nlm.nih.gov/34428039/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/34428039/
Selectivity Number of Off-targets
0