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PDD00017273 | PDD00017273 : Inhibitor of PARG
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 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
PARG
  • IC50:26 nM
  • IC50:37 nM
Inhibitor
Up to 10 uM, or 10X the cellular IC50 depending on the cell line

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Biochemical PAR chain persistence assay
Selectivity Assessment Description:
Biochemical selectivity against safety targets (% inhibition at 10 µM, binding assay Eurofins Panlab ...

Potency
Cellular
In Vitro

PARG

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acschembio.6b00609

Negative Control Compounds

N-Methyl-PDD00017273

Chemical Information

Molecular Formula C23H26N6O4S2
SMILEs Cc1cc(Cn2c(=O)n(Cc3cnc(C)s3)c(=O)c3cc(S(=O)(=O)NC4(C)CC4)ccc32)n(C)n1
InChI InChI=1S/C23H26N6O4S2/c1-14-9-16(27(4)25-14)12-28-20-6-5-18(35(32,33)26-23(3)7-8-23)10-19(20)21(30)29(22(28)31)13-17-11-24-15(2)34-17/h5-6,9-11,26H,7-8,12-13H2,1-4H3
Molecular weight 514.15 Da
AlogP 1.89744
HBond acceptors 10
HBond donors 1
Atoms 61

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 11 Jan 2017)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 27 Jan 2017)
Cellular Use Rating
PD00017273 is an inhibitor of human PARG enzyme with IC50 of 26 nM and good selectivity over the two closest functional homologues, PARP1 and ARH3 (>100 μM). It is suitable for use in cellular assays...
by SERP
(on 18 Apr 2017)
Cellular Use Rating
PDD00017273 is a potent inhibitor of PARG in cells (EC50=37 nM in a cellular PAR chain persistence assay) with little toxicity observed at 10 µM. While some degree of selectivity screening has been...
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