BY13 | BY13 : Degrader (PROTAC) of NCOA3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NCOA3
    • Dmax:71%
    • IC50:3-350 nM
    • DC50:31 nM
    Degrader (PROTAC)
    up to 1 uM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Global quantitative proteomics screen was conducted in LCC2 cells after 36 h of treatment with BY13. ...
    Selectivity Assessment Description:
    Both ERα and CDK4 protein levels were profoundly downregulated by BY13. BY13 containing pomalidomid ...

    Potency
    Cellular
    In Vitro

    NCOA3

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.5c00425

    In Vivo Validations

    Mouse
    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 3.44 ± 0.26 h
    Systemic clearance: 96.75 ± 31.97 mL/min/kg
    Cmax: 147.85 ± 54.69 ng/mL
    Area Under the Curve:: 318.39 ± 95.66 h*ng/mL
    Volume of Distribution at Steady-State: 29.14 ± 9.09 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.5c00425

    Dose: 4 mg/Kg
    Route of delivery: Intraperitoneal
    Plasma half life: 3.46 ± 0.53 h
    Cmax: 31.19 ± 4.6 ng/mL
    Tmax: 0.33 h
    Area Under the Curve:: 49.14 ± 11.7 h*ng/mL
    Bioavailability: 8%

    DOI Reference: 10.1021/acs.jmedchem.5c00425

    Dose: 20 mg/Kg
    Route of delivery: Oral
    Plasma half life: 4.49 ± 0.14 h
    Cmax: 25.44 ± 4.43 ng/mL
    Tmax: 0.33 h
    Area Under the Curve:: 47.07 ± 4.69 h*ng/mL
    Bioavailability: 1%

    DOI Reference: 10.1021/acs.jmedchem.5c00425

    Negative Control Compounds

    canSAR7437553
    Notes: At 1 uM, BY13-Neg was not able to significantly degrade SRC-3 in cells.

    Chemical Information

    Molecular Formula C35H35N9O4
    SMILEs C/C(=N\Nc1nc2ccccc2n1C1CN(C2CCN(c3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)C1)c1ccccn1
    InChI InChI=1S/C35H35N9O4/c1-21(25-8-4-5-16-36-25)39-40-35-37-26-9-2-3-10-27(26)43(35)23-19-42(20-23)22-14-17-41(18-15-22)28-11-6-7-24-31(28)34(48)44(33(24)47)29-12-13-30(45)38-32(29)46/h2-11,16,22-23,29H,12-15,17-20H2,1H3,(H,37,40)(H,38,45,46)/b39-21+
    Molecular weight 645.28 Da
    AlogP 3.194300000000001
    HBond acceptors 13
    HBond donors 2
    Atoms 83

    References

    Cross References

    Expert Reviews


    (on 23 Feb 2026 )
    Cellular Use Rating
    In Model Organisms
    This is a PROTAC (proteolysis-targeting chimera) that has high selectivity for the estrogen receptor signaling pathway and is an effective SRC-3 degrader, which exhibits significant inhibitory activity...
    (on 4 Mar 2026 )
    Cellular Use Rating
    In Model Organisms
    The recommended cellular concentration should be 1 uM as this consistently led to the degradation of SRC-3 in all cell lines tested. Inhibition can be achieved at lower concentrations, but degradation...
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