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HRO761 | HRO761 : allosteric inhibitor of WRN
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
WRN
  • IC50:100 nM
  • IC50:9 nM
  • IC50:Helicase activity
  • GI50:40 nM
  • GI50:40 nM
  • Activity:>80 -150 nM
allosteric
up to 1 µM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Proliferation inhibition of HRO761 for a panel of cell lines
In Vitro Selectivity Assessment
Potency Assay Off-Target:
HRO-761 was tested in biochemical assays against other helicases (RecQ helicases BLM, RecQ1 and RecQ ...

Potency
Cellular
In Vitro

WRN

Mode of Action: allosteric

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41586-024-07350-y

Chemical Information

Molecular Formula C31H31ClF3N9O5
SMILEs CCc1c(N2CCN(C(=O)c3ncnc(C)c3O)CC2)c(=O)n2nc(C3=CCOCC3)nc2n1CC(=O)Nc1ccc(C(F)(F)F)cc1Cl
InChI InChI=1S/C31H31ClF3N9O5/c1-3-22-25(41-8-10-42(11-9-41)28(47)24-26(46)17(2)36-16-37-24)29(48)44-30(39-27(40-44)18-6-12-49-13-7-18)43(22)15-23(45)38-21-5-4-19(14-20(21)32)31(33,34)35/h4-6,14,16,46H,3,7-13,15H2,1-2H3,(H,38,45)
Molecular weight 701.21 Da
AlogP 0.0
HBond acceptors 14
HBond donors 2
Atoms 80

Expert Reviews

by SERP
(on 8 Aug 2024 )
Cellular Use Rating
HRO761 is a potent allosteric inhibitor of WRN helicase. Despite it's high molecular weight and expected limitations in aqueous solubility, HRO761 has a convincing overall profile. It's selective activity...
by SERP
(on 11 Aug 2024 )
Cellular Use Rating
( The reviewer did not leave any comments )
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