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GNE-7883 | GNE-7883 : Allosteric inhibitor of TEAD1, TEAD2, TEAD3, TEAD4
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
TEAD1
  • IC50:4 nM
  • IC50:5 nM
  • IC50:2 nM
  • EC50:170 nM
  • EC50:290 nM
  • INH:3 uM
TEAD2
  • IC50:1 nM
  • IC50:1 nM
  • IC50:1 nM
    TEAD3
    • IC50:9 nM
    • IC50:10 nM
    • IC50:5 nM
      TEAD4
      • IC50:3 nM
      • IC50:3 nM
      • IC50:1 nM
        Allosteric
        3 µM

        Selectivity

        In Cell Selectivity Assessment
        Potency Assay Off-Target:
        mRNA-sequencing in OVCAR-8 and HCC1576 cells shows that GNE7883 selectively modulate YAP/TAZ target ...

        Potency
        Cellular
        In Vitro

        TEAD1

        Mode of Action: Allosteric

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1038/s43018-023-00577-0

        TEAD2

        Mode of Action: Allosteric

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1038/s43018-023-00577-0

        TEAD3

        Mode of Action: Allosteric

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1038/s43018-023-00577-0

        TEAD4

        Mode of Action: Allosteric

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1038/s43018-023-00577-0

        In Vivo Validations

        Mouse
        Dose: 250 mg/Kg
        Route of delivery: Subcutaneous
        Target engagement assay: tumor growth inhibition (TGI) of 102% in the mesothelioma NCIH226 xenograft mouse model

        DOI Reference: 10.1038/s43018-023-00577-0

        Chemical Information

        Molecular Formula C28H29FN6O2
        SMILEs Cc1nccnc1-c1nn2c(=O)cc(-c3ccc(C4CCCCC4)cc3)[nH]c2c1C(=O)N1CC(CF)C1
        InChI InChI=1S/C28H29FN6O2/c1-17-25(31-12-11-30-17)26-24(28(37)34-15-18(14-29)16-34)27-32-22(13-23(36)35(27)33-26)21-9-7-20(8-10-21)19-5-3-2-4-6-19/h7-13,18-19,32H,2-6,14-16H2,1H3
        Molecular weight 500.23 Da
        AlogP 0.0
        HBond acceptors 8
        HBond donors 1
        Atoms 66

        References

        Publications

        Cross References

        canSARChEMBLPDB

        Vendors

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        Expert Reviews

        by SERP
        (on 11 Aug 2023 )
        Cellular Use Rating
        In Model Organisms
        Through careful biophysical characterization, GNE-7883 was shown to interact specifically with TEAD at its lipid binding site, allosterically preventing interactions at a specific protein-protein interface...
        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