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AZD5305 | AZD5305 : Inhibitor of PARP1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PARP1
  • IC50:3 nM
  • Ki:0.13 nM
  • IC50:2 nM
  • IC50:2.3 nM
Inhibitor
100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
PARP Family Proteomic Data demonstrate that AZD5305 is highly selective for PARP1 over the other mem ...

Potency
Cellular
In Vitro

PARP1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.1c01012

In Vivo Validations

Mouse
Dose: 10, 1, 0.1, and 0.03 mg/kg
Route of delivery: Oral
Plasma half life: 8 h
Systemic clearance: 0.23 mL/min/kg
Fb : 99.927%
Bioavailability: 77%
Volume of Distribution at Steady-State: 0.17 L/Kg

DOI Reference: 10.1021/acs.jmedchem.1c01012

Rat
Dose: 10, 1, 0.1, and 0.03 mg/kg
Route of delivery: Oral
Plasma half life: 4.6 h
Systemic clearance: 1.1 mL/min/kg
Fb : 99.968%
Bioavailability: 132%
Volume of Distribution at Steady-State: 0.38 L/Kg

DOI Reference: 10.1021/acs.jmedchem.1c01012

Dog
Dose: 10, 1, 0.1, and 0.03 mg/kg
Route of delivery: Oral
Plasma half life: 10 h
Systemic clearance: 0.35 mL/min/kg
Fb : 99.83%
Bioavailability: 73%
Volume of Distribution at Steady-State: 0.3 L/Kg

DOI Reference: 10.1021/acs.jmedchem.1c01012

Monkey (Cynomolgus)
Dose: 10, 1, 0.1, and 0.03 mg/kg
Route of delivery: Oral
Plasma half life: 7.1 h
Systemic clearance: 0.84 mL/min/kg
Fb : 99.957%
Bioavailability: 122%
Volume of Distribution at Steady-State: 0.38 L/Kg

DOI Reference: 10.1021/acs.jmedchem.1c01012

Orthogonal Probes def

Niraparib
Veliparib

Chemical Information

Molecular Formula C22H26N6O2
SMILEs CCc1cc2ncc(CN3CCN(c4ccc(C(=O)NC)nc4)CC3)cc2[nH]c1=O
InChI InChI=1S/C22H26N6O2/c1-3-16-11-19-20(26-21(16)29)10-15(12-24-19)14-27-6-8-28(9-7-27)17-4-5-18(25-13-17)22(30)23-2/h4-5,10-13H,3,6-9,14H2,1-2H3,(H,23,30)(H,26,29)
Molecular weight 406.21 Da
AlogP 0.0
HBond acceptors 8
HBond donors 2
Atoms 56

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 1 May 2023 )
Cellular Use Rating
In Model Organisms
AZD5305 is one of the most PARP1 potent and selective inhibitors against other PARPs with high physicochemical and DMPK profiles, so it should be the great compound to evalutate PARP1 biology.
by SERP
(on 15 May 2023 )
Cellular Use Rating
In Model Organisms
AZD5305 is a highly potent PARP1 inhibitor that functions through the PARP-DNA trapping mechanism. It is highly selective against PARP2, exhibiting cytotoxic effects in a PARP1-dependent and PARP2-independent...
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