Compound name
AZD0156
Protein family
Protein Kinase
Target name
ATM
Affinity biochemical (nM)
0.04
Affinity on-target cellular (nM)
0.57
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002900a
SMILES
O=C(N(C1=C2C3=CC(C4=CC=C(N=C4)OCCCN(C)C)=CC=C3N=C1)C)N2C5CCOCC5
InChIKey
AOTRIQLYUAFVSC-UHFFFAOYSA-N
NCBI gene ID
472
UniProt ID
Q13315
Synonyms
TEL1, TELO1
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
HTRF assay
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896
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://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
397
Selectivity remarks
Screened at 1 µM, closest targets as % of control: GSG2 (33%), PIK3CA (36%), PIK4CB (30%), LRRK2 (13%), MTOR (7.4%), full screening data are available as supporting information, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-cellular potency (Immunoblot assay, ATR dependent phosphorylation of CHEK1 at Ser345, using HT-29 cells): IC50(ATR) = 6.2 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-cellular potency (ELISA, PIK3CA dependent phosphorylation of AKT1 at Thr308 using BT474 cells): IC50(PIK3CA) = 1.4 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-cellular potency (Immunoblot assay, MTOR dependent phosphorylation of AKT1 at Ser473 using MDA-MB-468 cells): IC50(MTOR) = 0.61 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(DNAPK) = 0.14 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(MTOR) = 0.20 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CA) = 0.32 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CB) = 1.8 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CG) = 1.1 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CD) = 0.27 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-cellular potency (Immunoblot assay, ATR dependent phosphorylation of CHEK1 at Ser345, using HT-29 cells): IC50(ATR) = 6.2 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-cellular potency (ELISA, PIK3CA dependent phosphorylation of AKT1 at Thr308 using BT474 cells): IC50(PIK3CA) = 1.4 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-cellular potency (Immunoblot assay, MTOR dependent phosphorylation of AKT1 at Ser473 using MDA-MB-468 cells): IC50(MTOR) = 0.61 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(DNAPK) = 0.14 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(MTOR) = 0.20 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CA) = 0.32 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CB) = 1.8 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CG) = 1.1 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CD) = 0.27 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896#
Selectivity Number of Off-targets
1