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JNK2_3 COV56d | JNK2/3 COV56d : Covalent Inhibitor of MAPK9, MAPK10
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
MAPK9
  • IC50:25 nM
  • Kd:15 nM
  • IC50:830 nM
  • EC50:883 nM
MAPK10
  • IC50:40 nM
  • Kd:5 nM
  • IC50:1909 nM
    Covalent Inhibitor
    up to 5 uM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Selective 11x over JNK1 as confirmed by NanoBRET
    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Kinome screening was carried out in a representative panel consisting of 97 kinases (scanEDGE─KINOME ...

    Potency
    Cellular
    In Vitro

    MAPK9

    Mode of Action: Covalent Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.5c00884

    MAPK10

    Mode of Action: Covalent Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.5c00884

    Orthogonal Probes def

    CTx-0294885

    Chemical Information

    Molecular Formula C30H24N6O3
    SMILEs C=CC(=O)Nc1cccc(C(=O)Nc2cccc(-n3cc(NC(=O)Nc4cccc5ccccc45)cn3)c2)c1
    InChI InChI=1S/C30H24N6O3/c1-2-28(37)32-22-11-5-10-21(16-22)29(38)33-23-12-7-13-25(17-23)36-19-24(18-31-36)34-30(39)35-27-15-6-9-20-8-3-4-14-26(20)27/h2-19H,1H2,(H,32,37)(H,33,38)(H2,34,35,39)
    Molecular weight 516.19 Da
    AlogP 6.046300000000004
    HBond acceptors 9
    HBond donors 4
    Atoms 63

    References

    Publications

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    Expert Reviews

    by SERP
    (on 17 Aug 2025)
    Cellular Use Rating
    In cell based assays, JNK2_3 Cov56d should provide selective inhibition of JNK2 verse JNK1 when used at concentrations of 1-5 uM. However, the potency of the probe against JNK3 in cells in not known and...
    by SERP
    (on 21 Aug 2025)
    Cellular Use Rating
    56d is likely a useful compound to probe MAPK9 and 10 (JNK2 and 3) function. It has an ATP-competitive, covalent mechanism of action with impressive kinact/KI. This compound shows very limited in vitro...
    by SERP+
    (on 9 Jul 2026)
    Cellular Use Rating
    JNK2_3 COV56d is a selective chemical probe for JNK2 and JNK3 with in vitro inhibition and selectivity over JNK1. It also has selectivity against other 95 kinases but selectivity against the rest of the...
    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