Chemical Probes logo
AZD0156 | AZD0156 : Inhibitor of ATM
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ATM
  • IC50:0.04 nM
  • IC50:0.57 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Kinome selectivity data generated using DiscoveRx KINOMEscan™ screening platform with AZD0156 screen ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
ATR cell. IC50 = 6.2 µM, mTOR cell IC50 = 0.61 µM, PI3Ka IC50 = 1.4 µM

Potency
Cellular
In Vitro

ATM

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.7b01896

In Vivo Validations

Rat
Dose:
Route of delivery: Oral
Plasma half life: 4.4 h
Systemic clearance: 15.5 mL/min/kg
Bioavailability: 57%
Volume of Distribution at Steady-State: 4.3 L/kg

DOI Reference: 10.1021/acs.jmedchem.7b01896

Dog
Dose:
Route of delivery: Oral
Plasma half life: 7.6 h
Systemic clearance: 33.3 mL/min/kg
Bioavailability: 54%
Volume of Distribution at Steady-State: 17.6 L/kg

DOI Reference: 10.1021/acs.jmedchem.7b01896

Mouse
Dose: 5 mg/Kg
Route of delivery: Oral
Target engagement assay: Immunocompromised mice SW620 xenograft model in combination with irinotecan. Or immunocompromised mice bearing HBCx-10 patient derived tumors in combination with olaparib.

DOI Reference: 10.1021/acs.jmedchem.7b01896

Chemical Information

Molecular Formula C26H31N5O3
SMILEs CN(C)CCCOc1ccc(-c2ccc3ncc4c(c3c2)n(C2CCOCC2)c(=O)n4C)cn1
InChI InChI=1S/C26H31N5O3/c1-29(2)11-4-12-34-24-8-6-19(16-28-24)18-5-7-22-21(15-18)25-23(17-27-22)30(3)26(32)31(25)20-9-13-33-14-10-20/h5-8,15-17,20H,4,9-14H2,1-3H3
Molecular weight 461.24 Da
AlogP 0.0
HBond acceptors 8
HBond donors --
Atoms 65

References

Publications

Cross References

canSARChEMBLChEMBLBindingDB

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 26 Jan 2024 )
Cellular Use Rating
In Model Organisms
The imidazo[4,5-c]quinolin-2-one derivative, AZD-0156, is an exceptionally potent ATM inhibitor, with both picomolar activity in vitro (IC50 = 0.04 nM) and in cells (IC50 = 0.57 nM). AZD-0156 was profiled...
by SERP
(on 12 Feb 2024 )
Cellular Use Rating
In Model Organisms
This compound is a potent in vitro and in vivo tool compound for assessing ATM with high kinase selectivity. While prior analogs were beneficial for in vitro profiling, this compound is suitable for in...
by SERP
(on 15 Feb 2024 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria