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AZ191 | Inhibitor of DYRK1B
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
DYRK1B
  • IC50:17 nM
Inhibitor
20 nM - 3 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - DYRK1A 88 nM, DYRK2 1,890 nM

Potency Assay Off-Target:
In vitro radioactivity-based substrate phosphorylation assay
Selectivity Assessment Description:
In Kinomescan (DiscoverX) assessing >400 kinases, there were only 8 non-mutated kinase hits at ...

Potency
Cellular
In Vitro

DYRK1B

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Chemical Information

Molecular Formula C24H27N7O
SMILEs COc1cc(N2CCN(C)CC2)ccc1Nc1nccc(-c2cn(C)c3cnccc23)n1
InChI InChI=1S/C24H27N7O/c1-29-10-12-31(13-11-29)17-4-5-21(23(14-17)32-3)28-24-26-9-7-20(27-24)19-16-30(2)22-15-25-8-6-18(19)22/h4-9,14-16H,10-13H2,1-3H3,(H,26,27,28)
Molecular weight 429.23 Da
AlogP 0.0
HBond acceptors 8
HBond donors 1
Atoms 59

References

Publications

    Cross References

    canSARChEMBLBindingDBPDBPubMed

    Vendors

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    Expert Reviews

    by SERP
    (on 20 May 2016 )
    Cellular Use Rating
    This compound is too promiscuous kinome-wide to be useful as a cellular inhibitor of DYRK1B.
    by SERP
    (on 26 May 2016 )
    Cellular Use Rating
    AZ191 is claimed to have 5-10x selectivity over DYRK1A and >100x over DYRK2. This molecule has been tested against >400 kinases at 1 uM and only hits 9 of them. A range of cellular effects are reported...
    by SERP
    (on 15 Jun 2016 )
    Cellular Use Rating
    Concentrations higher than a few micromolar are likely to inhibit other kinases.
    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