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AZ2858 | AZ2858 : Inhibitor of GSK3B
RATINGS:
Cellular Use: (1 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
GSK3B
  • Ki:4.9 nM
  • IC50:76 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
AZD2858 was evaluated for pan-kinase selectivity (10 μM). The compound shows a good overall selectiv ...

Potency
Cellular
In Vitro

GSK3B

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm201724m

Chemical Information

Molecular Formula C21H23N7O3S
SMILEs CN1CCN(S(=O)(=O)c2ccc(-c3cnc(N)c(C(=O)Nc4cccnc4)n3)cc2)CC1
InChI InChI=1S/C21H23N7O3S/c1-27-9-11-28(12-10-27)32(30,31)17-6-4-15(5-7-17)18-14-24-20(22)19(26-18)21(29)25-16-3-2-8-23-13-16/h2-8,13-14H,9-12H2,1H3,(H2,22,24)(H,25,29)
Molecular weight 453.16 Da
AlogP 0.0
HBond acceptors 10
HBond donors 3
Atoms 55

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

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Expert Reviews

by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
This is a potent compounds (4.9 nM in vitro) and a decent selectivity of 110 fold in the panel tested. However, the selectivity has only been assessed versus 26 kinases. Using an orthogonal probe is therefore...

Portal Comments

Note that AZ2858 was not specifically assessed for its binding to the related GSK3A

(last updated: 24 Jan 2023)

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