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A1874 | A1874 : Degrader (PROTAC) of BRD4
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 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
BRD4
    • DC50:32 nM
    • IC50:86.3 nM
    • Dmax:98%
    100 nM to 1 µM
    100 nM

    Selectivity

    Potency
    Cellular
    In Vitro

    BRD4

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1158/0008-5472.CAN-18-2918

    Negative Control Compounds

    A1875
    Notes: A1875, a diastereomeric analogue of A1874 with greatly reduced affinity for MDM2, had substantially diminished effectiveness in MTS assay.

    Orthogonal Probes def

    dBET6
    AT1
    MZ1

    Chemical Information

    Molecular Formula C58H62Cl3F2N9O7S
    SMILEs COc1cc(C(=O)NCCOCCOCCOCCNC(=O)C[C@@H]2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F
    InChI InChI=1S/C58H62Cl3F2N9O7S/c1-32-33(2)80-56-48(32)51(35-11-14-37(59)15-12-35)67-44(53-71-70-34(3)72(53)56)29-47(73)65-19-21-77-23-25-79-26-24-78-22-20-66-54(74)36-13-18-43(45(27-36)76-7)68-55(75)52-49(39-9-8-10-41(61)50(39)63)58(31-64,46(69-52)30-57(4,5)6)40-17-16-38(60)28-42(40)62/h8-18,27-28,44,46,49,52,69H,19-26,29-30H2,1-7H3,(H,65,73)(H,66,74)(H,68,75)/t44-,46-,49-,52+,58-/m0/s1
    Molecular weight 1171.35 Da
    AlogP 10.339739999999995
    HBond acceptors 16
    HBond donors 4
    Atoms 142

    Vendors

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    Expert Reviews

    by SERP+
    (on 20 Feb 2025)
    Cellular Use Rating
    This is a potent degrader of BRD4. Although many BRD4 PROTACS exist, this is one of the first to use MDM2 as the E3 ligase. MDM2-mediated degradation has been demonstrated via control experiments. However,...
    by SERP+
    (on 6 Feb 2026)
    Cellular Use Rating
    This paper identifies a potent MDM2 recruiting PROTAC with nanomolar DC50 and high Dmax reported. Demonstration of identify ternary complex formation would have been desirable. The compound has some potential...
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