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SB-216763 | SB-216763 : ATP competitive inhibitor of GSK3A, GSK3B
RATINGS:
Cellular Use: (3 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
GSK3A
  • IC50:34 nM
  • Ki:9 nM
  • EC50:3.6 uM
GSK3B
  • Inhibition:96%
    ATP competitive
    5 µM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    The selectivity of SB-216763 was investigated by testing the ability of this compound to inhibit a p ...
    Selectivity Assessment Description:
    KinomeSCAN at 10 uM

    Potency
    Cellular
    In Vitro

    GSK3A

    Mode of Action: ATP competitive

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/s1074-5521(00)00025-9

    GSK3B

    Mode of Action: ATP competitive

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1016/s1074-5521(00)00025-9

    Chemical Information

    Molecular Formula C19H12Cl2N2O2
    SMILEs Cn1cc(C2=C(c3ccc(Cl)cc3Cl)C(=O)NC2=O)c2ccccc21
    InChI InChI=1S/C19H12Cl2N2O2/c1-23-9-13(11-4-2-3-5-15(11)23)17-16(18(24)22-19(17)25)12-7-6-10(20)8-14(12)21/h2-9H,1H3,(H,22,24,25)
    Molecular weight 370.03 Da
    AlogP 4.0523000000000025
    HBond acceptors 4
    HBond donors 1
    Atoms 37

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    Expert Reviews

    by SERP+
    (on 22 Mar 2023 )
    Cellular Use Rating
    Improved analogues exist with higher potency and more diverse kinase profiling (98 kinases). The compound shows a large drop-off in the cellular assay compared to the measured in vitro potency due to the...
    by SERP
    (on 21 Apr 2023 )
    Cellular Use Rating
    SB-216763 is a potent GSK3a/b inhibitor with high levels of selectivity against 24 related kinases. Broader selectivity across the kinome and proteome is not as well established. This probe has been used...
    by SERP+
    (on 17 Jun 2024 )
    Cellular Use Rating
    This compound in has a cellular potency of 3,6 µM. No direct target engagement assay has been applied for profiling the compound. The selectivity has only been assessed for 25 kinases. No cytotoxicity...
    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