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BRD9-PROTAC-E5 | BRD9-PROTAC-E5 : Degrader (PROTAC) of BRD9
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BRD9
    • IC50:0.27 ± 0.02 nM
    • DC50:0.016 nM
    • Dmax:97%
    Degrader (PROTAC)
    up to 10 nM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    PROTAC E5 did not induce the degradation of BRD4 and BRD7 in MV4-11 cells up to 100 nM. E5 had excel ...

    Potency
    Cellular
    In Vitro

    BRD9

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.4c00883

    In Vivo Validations

    Mouse
    Dose: 20 mg/Kg
    Route of delivery: Intragastric
    Plasma half life: 19.22 h
    Cmax: 126.98 ng/mL
    Tmax: 1.00 h
    Area Under the Curve:: 1297.06 h·ng/mL

    DOI Reference: 10.1021/acs.jmedchem.4c00883

    Chemical Information

    Molecular Formula C46H49N5O6
    SMILEs COc1cc(-c2cn(C)c(=O)c3ccccc23)cc(OC)c1CN1CCC(CN2CCC(c3ccc4c5c(cccc35)C(=O)N4C3CCC(=O)NC3=O)CC2)CC1
    InChI InChI=1S/C46H49N5O6/c1-48-26-36(32-7-4-5-8-34(32)45(48)54)30-23-40(56-2)37(41(24-30)57-3)27-50-19-15-28(16-20-50)25-49-21-17-29(18-22-49)31-11-12-38-43-33(31)9-6-10-35(43)46(55)51(38)39-13-14-42(52)47-44(39)53/h4-12,23-24,26,28-29,39H,13-22,25,27H2,1-3H3,(H,47,52,53)
    Molecular weight 767.37 Da
    AlogP 6.232900000000006
    HBond acceptors 11
    HBond donors 1
    Atoms 106

    References

    Publications

    Cross References

    Expert Reviews

    by SERP
    (on 30 Jul 2024 )
    Cellular Use Rating
    In Model Organisms
    In some cell lines, the compound is less effective (SU-DHL-6 (374nM) and U937 (1um))
    by SERP+
    (on 6 Feb 2026 )
    Cellular Use Rating
    In Model Organisms
    This is a decent BRD9 degrader. Some additional proteins are downregulated as seen in proteomic experiments after 24 h at 0.33nM and it is not clear if these are effects from brd9 degradation or off-target...
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