Compound name
AZD 7648
Protein family
Protein Kinase
Target name
PRKDC
Affinity biochemical (nM)
0.6
Affinity on-target cellular (nM)
91.3
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001783a
SMILES
Cc1cc2ncnn2cc1Nc1ncc2c(n1)n(C1CCOCC1)c(=O)n2C
InChIKey
XISVSTPEXYIKJL-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
Biochemical assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/31699977/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
ELISA (inhibition of DNA-PKcs autophosphorylation at Ser2056 in IR-treated A549 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/31699977/
Affinity on-target cellular relation
=
Selectivity platform
SelectScreen (Kinase Profiling Service, ThermoFisher)
Selectivity platform number of targets
397
Selectivity remarks
Screened at 1 µM, closest target with >50% of inhibtion:PIK3KA, PIK3KD, PIK3G; In-vitro follow-up of cloestes targets in biochemical assays: IC50(PIK3KA) >60 nM, IC50(PIK3KD) >60 nM, IC50(PIK3G) = 37.8 nM, https://pubmed.ncbi.nlm.nih.gov/31699977/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/31699977/
Selectivity Number of Off-targets
3