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DOT1L808 | DOT1L808 : Degrader (PROTAC) of DOT1L
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DOT1L
    • DC50:5 nM
    • DC50:6.5 nM
    • IC50:46.6 nM
    10-100 nM
    up to 300 nM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Global proteomics of DOT1L808 in MOLT4 cells. Cells were treated with 100 nM DOT1L808 for 5 h.

    Potency
    Cellular
    In Vitro

    DOT1L

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.5c03128

    In Vivo Validations

    Mouse
    Dose: 2 mg/Kg
    Route of delivery: Intraperitoneal
    Plasma half life: 5.2 h
    Cmax: 1.6 μM
    Area Under the Curve:: 10.8 μM*hr

    DOI Reference: 10.1021/acs.jmedchem.5c03128

    Chemical Information

    Molecular Formula C61H72ClF3N14O9S2
    SMILEs Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCN2CCN(CCN3CCN(c4ncnc(Nc5cc(S(C)(=O)=O)ccc5N[C@@H](c5cccc6c5OC(F)(F)O6)c5ncccc5Cl)n4)CC3)CC2)c1
    InChI InChI=1S/C61H72ClF3N14O9S2/c1-37-52(89-36-70-37)38-11-12-39(33-67-54(81)46-31-40(80)34-79(46)55(82)53(59(2,3)4)73-56(83)60(63)15-16-60)48(30-38)86-29-28-77-22-20-75(21-23-77)18-19-76-24-26-78(27-25-76)58-69-35-68-57(74-58)72-45-32-41(90(5,84)85)13-14-44(45)71-49(50-43(62)9-7-17-66-50)42-8-6-10-47-51(42)88-61(64,65)87-47/h6-14,17,30,32,35-36,40,46,49,53,71,80H,15-16,18-29,31,33-34H2,1-5H3,(H,67,81)(H,73,83)(H,68,69,72,74)/t40-,46+,49+,53-/m1/s1
    Molecular weight 1300.47 Da
    AlogP 6.451620000000007
    HBond acceptors 23
    HBond donors 5
    Atoms 162

    References

    Publications

    Cross References

    canSAR: 7719212 canSAR: 15

    Expert Reviews

    by SERP
    (on 7 Apr 2026)
    Cellular Use Rating
    In Model Organisms
    DOT1L808 is a high quality chemical probe for studying DOT1L. It displays potent on-target activity (DC₅₀ = 5 nM), exceptional proteome-wide selectivity (degradation selectivity validated by proteomics),...
    If you would like to explore AI-generated evaluations, you may wish to visit the page for this compound on our collaborator website
    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