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EP300-Deg-25a | EP300-Deg-25a : Degrader (PROTAC) of EP300, CREBBP
RATINGS:
Cellular Use: (2 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
EP300
  • Inhibition:25.1%
  • Dmax:90.8 ± 1.1%
CREBBP
    • Dmax:59.6 ± 6.9%
    1 µM
    up to 1 uM, no hook effect up to 10 uM

    Selectivity

    Potency
    Cellular
    In Vitro

    EP300

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acsmedchemlett.6c00153

    CREBBP

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acsmedchemlett.6c00153

    Chemical Information

    Molecular Formula C46H50N10O9
    SMILEs O=C1CCC(N2C(=O)c3cccc(NCCOCCOCCn4cc(COc5ccc(C6(C(=O)N7CCC[C@H]7C(=O)Nc7cccc8[nH]ncc78)CCCC6)cc5)nn4)c3C2=O)C(=O)N1
    InChI InChI=1S/C46H50N10O9/c57-39-16-15-38(42(59)50-39)56-43(60)32-6-3-9-36(40(32)44(56)61)47-19-22-63-24-25-64-23-21-54-27-30(51-53-54)28-65-31-13-11-29(12-14-31)46(17-1-2-18-46)45(62)55-20-5-10-37(55)41(58)49-34-7-4-8-35-33(34)26-48-52-35/h3-4,6-9,11-14,26-27,37-38,47H,1-2,5,10,15-25,28H2,(H,48,52)(H,49,58)(H,50,57,59)/t37-,38?/m0/s1
    Molecular weight 886.38 Da
    AlogP 3.7214000000000027
    HBond acceptors 19
    HBond donors 4
    Atoms 115

    References

    Publications

    Cross References

    canSAR: 7719213 canSAR: 16

    Expert Reviews

    by SERP
    (on 26 Aug 2026)
    Cellular Use Rating
    Compound 25a, a proline-based, cereblon-recruiting PROTAC, was identified as a degrader that preferentially promotes degradation of EP300 (p300) over its close paralog, CBP. EP300 is a lysine acetyltransferase...
    by SERP
    (on 31 Aug 2026)
    Cellular Use Rating
    The PROTAC EP300-Deg-25a degrades effectively degrades EP300 while largely sparing its close homolog CPB at low micromolar concentrations. Further selectivity data (e.g. global proteomics) and broader...
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