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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 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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