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WZ4003 | Inhibitor of NUAK1, NUAK2
RATINGS:
Cellular Use: (3 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...
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