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TH1760 | Inhibitor of NUDT15
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
NUDT15
  • IC50:25 nM
  • IC50:57 nM
  • ΔTm:+7 ºC
Inhibitor
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
@ 100 uM, TH1760 showed selectivity over a panel of related proteins with sequential or functional r ...
Selectivity Assessment Description:
The selectivity of TH1760 was further scrutinized and confirmed with the Eurofins Cerep SafetyScreen ...

Potency
Cellular
In Vitro

NUDT15

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41589-020-0592-z

Chemical Information

Molecular Formula C20H18N4O5S
SMILEs O=C(c1ccc2[nH]ccc2c1)N1CCN(S(=O)(=O)c2ccc3[nH]c(=O)oc3c2)CC1
InChI InChI=1S/C20H18N4O5S/c25-19(14-1-3-16-13(11-14)5-6-21-16)23-7-9-24(10-8-23)30(27,28)15-2-4-17-18(12-15)29-20(26)22-17/h1-6,11-12,21H,7-10H2,(H,22,26)
Molecular weight 426.10 Da
AlogP 1.7491
HBond acceptors 9
HBond donors 2
Atoms 48

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Expert Reviews

by SERP
(on 2 Dec 2020 )
Cellular Use Rating
This is a top-quality chemical probe for in vitro and cellular studies of NUDT15. Nanomolar affinity to NUDT15 is shown, and direct engagement with the protein has clearly been demonstrated (TSA, X-ray)....
by SERP
(on 2 Dec 2020 )
Cellular Use Rating
TH1760 chemical probe for NUDT15 was extensively characterized in vitro and in cells. It is highly potent in vitro and shows a remarkable selectivity within the Nudix enzyme family. The cellular characterization...
by SERP
(on 8 Dec 2020 )
Cellular Use Rating
In Model Organisms
Sufficient efforts have been made to characterize the lead compound and compare it with its negative control, which is structurally similar to the parental by the difference of a methyl group at a key...
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