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TAO Kinase inhibitor 1 | TAO Kinase inhibitor 1 : Inhibitor of TAOK1, TAOK2
RATINGS:
Cellular Use: (3 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
TAOK1
  • IC50:11 nM
  • IC50:10 uM
TAOK2
  • IC50:15 nM
    Inhibitor
    10 µM
    up to 30 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    In vitro kinase assays at 300 nM CP43 using 70 different kinases. TAOK1 8%, TAOK2 11%, TAOK3 13% ret ...

    Potency
    Cellular
    In Vitro

    TAOK1

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1158/1535-7163.MCT-17-0077

    TAOK2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1158/1535-7163.MCT-17-0077

    Chemical Information

    Molecular Formula C25H24N2O2
    SMILEs O=C(CNC(=O)c1ccc(-c2ccccc2)cc1)NC1CCCc2ccccc21
    InChI InChI=1S/C25H24N2O2/c28-24(27-23-12-6-10-20-9-4-5-11-22(20)23)17-26-25(29)21-15-13-19(14-16-21)18-7-2-1-3-8-18/h1-5,7-9,11,13-16,23H,6,10,12,17H2,(H,26,29)(H,27,28)
    Molecular weight 384.18 Da
    AlogP 4.277200000000003
    HBond acceptors 4
    HBond donors 2
    Atoms 53

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    Expert Reviews

    by SERP
    (on 9 Nov 2022 )
    Cellular Use Rating
    ( The reviewer did not leave any comments )
    by SERP+
    (on 22 Mar 2023 )
    Cellular Use Rating
    TAO1 Kinase Inhibitor is the only available probe for TOAK1/2. There are potential concerns about the selectivity of the probe over other kinases, as the in-vitro selectivity panel only consists of 70...
    by SERP+
    (on 17 Jun 2024 )
    Cellular Use Rating
    The presented inhibitor displays high in vitro potency with 11 nM and 15 nM for TAOK1 and TAOK2, respectively. However, selectivity assessment is limited with only 70 kinases having been tested. Already,...
    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