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CRBN-6-5-5-VHL | CRBN-6-5-5-VHL : Degrader, PROTAC of CRBN
RATINGS:
Cellular Use: (3 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
CRBN
    • DC50:1.5 nM
    Degrader (PROTAC)
    5-10 nM for measuring degradation and 50-100nM to study downstream effects
    100-1000 nM

    Selectivity

    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    IKZF1 (Ikaros) and IKZF3 (Aiolos) are transcription factors and neosubstrates of Cereblon. Applicati ...

    Potency
    Cellular
    In Vitro

    CRBN

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1039/c8cc09541h

    Negative Control Compounds

    (-)CRBN-6-5-5-VHL
    (*)CRBN-6-5-5-VHL
    CRBN-6-5-5-VHL(-)
    (-)CRBN-6-5-5-VHL(-)

    Chemical Information

    Molecular Formula C51H69N7O10S
    SMILEs Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCOCCCCCOCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1
    InChI InChI=1S/C51H69N7O10S/c1-33-44(69-32-54-33)35-20-18-34(19-21-35)30-53-46(62)40-29-36(59)31-57(40)50(66)45(51(2,3)4)55-41(60)17-8-13-28-68-27-12-7-11-26-67-25-10-6-5-9-24-52-38-16-14-15-37-43(38)49(65)58(48(37)64)39-22-23-42(61)56-47(39)63/h14-16,18-21,32,36,39-40,45,52,59H,5-13,17,22-31H2,1-4H3,(H,53,62)(H,55,60)(H,56,61,63)/t36-,39?,40+,45-/m1/s1
    Molecular weight 971.48 Da
    AlogP 5.674920000000003
    HBond acceptors 17
    HBond donors 5
    Atoms 138

    References

    Publications

    Cross References

    canSARChEMBL

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    Expert Reviews

    by SERP
    (on 16 Feb 2021)
    Cellular Use Rating
    In Model Organisms
    This is a good probe that can be used to study the CRBN degradation. The in vivo properties of this molecule still need to be evaluated or improved.
    by SERP
    (on 26 Feb 2021)
    Cellular Use Rating
    The compound is highly potent at very low nanomolar range.
    by SERP
    (on 9 Apr 2021)
    Cellular Use Rating
    (The reviewer did not leave any public comments)
    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