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Olaparib | Olaparib : Inhibitor of PARP1 and PARP
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
  • IC 50:5 nM
  • IC 50:1.4 nM
  • IC 50:6 nM
PARP2
  • IC 50:1 nM
  • IC 50:12.3 nM
  • IC 50:6 nM
Inhibitor
10-300 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - TNKS 1.5 uM, PARP3 230 nM, PARP4 410 nM, TNKS1 1230 nM, PARP10 1250 nM

Potency Assay Off-Target:
In vitro activity assay with biotinylated-NAD. In in vitro ADP ribosylation assays, oliparib was onl ...
Selectivity Assessment Description:
In vitro activity assay with biotinylated-NAD. In in vitro ADP ribosylation assays, olaparib was onl ...

Potency
Cellular
In Vitro

PARP1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm8001263

PARP2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm8001263

In Vivo Validations

Mouse, Rat, Dog
Dose: 10 mg/kg (mouse) , 15 mg/kg (rat), 2.5 mg/kg (dog)
Route of delivery: Intravenous, Oral
Plasma half life: 53 min (rat, IV), 170 min (dog, IV)
Systemic clearance: 49 mL/min/kg (rat, IV), 5.4 mL/min/kg (dog, IV)
Organ of interest (O): SW620 xenograft
Target engagement assay: Not available

DOI Reference: 10.1021/jm8001263

Orthogonal Probes def

VELIPARIB
NIRAPARIB
TALAZOPARIB

Chemical Information

Molecular Formula C24H23FN4O3
SMILEs O=C(c1cc(Cc2n[nH]c(=O)c3ccccc23)ccc1F)N1CCN(C(=O)C2CC2)CC1
InChI InChI=1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30)
Molecular weight 434.18 Da
AlogP 0.0
HBond acceptors 7
HBond donors 1
Atoms 55

References

Publications

Cross References

canSARChEMBLBindingDBPDBGDSC1 GDSC1GDSC2

Vendors

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

Expert Reviews

by SERP
(on 1 Aug 2016 )
Cellular Use Rating
In Model Organisms
Olaparib provides an effective tool compound for investigating the role of the PARPs in DNA repair and other biological contexts. However, olaparib inhibits predominantly PARPs 1 and 2, leaving the...
by SERP
(on 20 Dec 2016 )
Cellular Use Rating
In Model Organisms
Olaparib is a PARP 1/2/3 inhibitor. This agent is an excellent tool to study PARP inhibition in both the cellular and in vivo setting. However, an important study about the mechanism of these probes...
Portal staff comment: A new publication appeared in December 2016 (PMID 28001384) indicating that veliparib and niraparib are more selective than olaparib among PARP family proteins.
by SERP
(on 15 Jun 2017 )
Cellular Use Rating
In Model Organisms
Olaparib has actvity against PARPs 1, 2, 3 and 4; it has little activity against other members of the PARP family.
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