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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
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DOT1L
    • DC50:5 nM
    • DC50:6.5 nM
    • IC50:46.6 nM
    Degrader (PROTAC)
    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

    Coming Soon...

    References

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    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),...
    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