Compound name
KU-60019
Protein family
Protein Kinase
Target name
ATM
Affinity biochemical (nM)
6.3
Affinity on-target cellular (nM)
150
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002933a
SMILES
C[C@@H]1O[C@@H](CN(CC(NC2=CC3=C(C=C2)SC4=C(C3)C=CC=C4C5=CC(C=C(O5)N6CCOCC6)=O)=O)C1)C
InChIKey
SCELLOWTHJGVIC-BGYRXZFFSA-N
NCBI gene ID
472
UniProt ID
Q13315
Synonyms
TEL1, TELO1
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/19808981/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Immunoblot assay (phosphorylation of ATM at Ser1981, using HT-29 cells)
Affinity on-target cellular source knowledge
https://aacrjournals.org/mct/article/19/1/13/274205/Pharmacology-of-the-ATM-Inhibitor-AZD0156
Affinity on-target cellular relation
=
Selectivity platform
Millipore KinaseProfiler
Selectivity platform number of targets
229
Selectivity remarks
Screened at 1 µM, closest targets as % of activity: FMS (46%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/19808981/;
Screened at 1 µM, PI3-Kinase HTRF assay, closest targets: PIK3CB (9%), PIK3CG (3%), screening data are not available in paper, https://pubmed.ncbi.nlm.nih.gov/19808981/;
In-vitro potency (enzymatic assay): IC50(DNAPK) = 17 µM, https://pubmed.ncbi.nlm.nih.gov/19808981/;
In-vitro potency (enzymatic assay): IC50(ATR) >10 µM, https://pubmed.ncbi.nlm.nih.gov/19808981/;
Screened at 1 µM, PI3-Kinase HTRF assay, closest targets: PIK3CB (9%), PIK3CG (3%), screening data are not available in paper, https://pubmed.ncbi.nlm.nih.gov/19808981/;
In-vitro potency (enzymatic assay): IC50(DNAPK) = 17 µM, https://pubmed.ncbi.nlm.nih.gov/19808981/;
In-vitro potency (enzymatic assay): IC50(ATR) >10 µM, https://pubmed.ncbi.nlm.nih.gov/19808981/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/19808981/
Selectivity Number of Off-targets
2