Compound name
AZD1390
Protein family
Protein Kinase
Target name
ATM
Affinity biochemical (nM)
0.09
Affinity on-target cellular (nM)
0.78
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0002901a
SMILES
O=C(N1C(C)C)N(C)C2=C1C3=CC(C4=CC=C(OCCCN5CCCCC5)N=C4)=C(F)C=C3N=C2
InChIKey
VQSZIPCGAGVRRP-UHFFFAOYSA-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://pubs.acs.org/doi/10.1021/acs.jmedchem.0c00766
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot assay (using NCI-H2228 cells and anti-ATM pS1981 (ab81292) antibody)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/29938225/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Thermo Fisher Scientific)
Selectivity platform number of targets
121
Selectivity remarks
Screened at 1 µM, closest targets with >50% of activity in the screen: CSF1R, NUAK1, SGK, screening data are not available in paper, https://pubmed.ncbi.nlm.nih.gov/29938225/;
Screened at 1 µM, against 125 kinases, Eurofins Panlabs screen, closest target with >50% of activity in the screen: FMS, screening data are not available in paper, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(ATR) >30 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(PIK3CA) >12 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(MTOR) >16.1 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(DNAPK) >29.9 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(HERG) = 6.55 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
Screened at 1 µM, against 125 kinases, Eurofins Panlabs screen, closest target with >50% of activity in the screen: FMS, screening data are not available in paper, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(ATR) >30 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(PIK3CA) >12 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(MTOR) >16.1 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(DNAPK) >29.9 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(HERG) = 6.55 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/29938225/
Selectivity Number of Off-targets
3