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WZ4003 | WZ4003 : Inhibitor of NUAK1, NUAK2
RATINGS:
Cellular Use: (4 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NUAK1
  • IC 50:20 nM
NUAK2
  • IC 50:100 nM
Inhibitor
Up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
No significant off-target activity was detected against 140 additional protein kinases at 1 uM.
Selectivity Assessment Description:
No significant off-target activity was detected against 140 additional protein kinases at 1 uM.
In Cell Selectivity Assessment
Potency Assay Off-Target:
In HEK-293 cells, WZ4003 did not inhibit phosphorylation of AMPK substrates.
Selectivity Assessment Description:
In HEK-293 cells, WZ4003 did not inhibit phosphorylation of AMPK substrates.

Potency
Cellular
In Vitro

NUAK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1042/BJ20131152

NUAK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1042/BJ20131152

Chemical Information

Molecular Formula C25H29ClN6O3
SMILEs CCC(=O)Nc1cccc(Oc2nc(Nc3ccc(N4CCN(C)CC4)cc3OC)ncc2Cl)c1
InChI InChI=1S/C25H29ClN6O3/c1-4-23(33)28-17-6-5-7-19(14-17)35-24-20(26)16-27-25(30-24)29-21-9-8-18(15-22(21)34-3)32-12-10-31(2)11-13-32/h5-9,14-16H,4,10-13H2,1-3H3,(H,28,33)(H,27,29,30)
Molecular weight 496.20 Da
AlogP 0.0
HBond acceptors 9
HBond donors 2
Atoms 64

References

Publications

Cross References

canSARChEMBLBindingDBGDSC2

Expert Reviews

by SERP
(on 6 May 2016)
Cellular Use Rating
No available PK or toxicology data; no way to judge whether or not it should be utilized in vivo. The probe is selective and has a target not well addressed by other molecules. Further work on physiochemistry,...
by SERP
(on 15 Jun 2016)
Cellular Use Rating
This appears to be a highly selective NUAK1 inhibitor without significant off-target actions at 140 other tested kinases. There are no data available for potential off-target actions at other druggable...
by SERP
(on 17 Jun 2016)
Cellular Use Rating
In Model Organisms
The compound has good kinase selectivity, but the cellular activity is not at the level I would consider useful for a bona fide probe (<1 uM). The authors have highlighted a few more potent compounds...
by SERP
(on 6 May 2026)
Cellular Use Rating
This probe was reported to be 20nM (Nuak1) and 100 nM (Nuak2). It is important to note that the reported NUAK IC50s were not done at the Km of ATP of these enzymes. Thus, we test WZ4003 at Km of ATP for...
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