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ML352 | ML352 : Non Competitive Inhibitor of SLC5A7
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 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
SLC5A7
    • IC50:90 - 266 nM
    • Activity:3% remaining
    • IC50:72 nM
    Inhibitor
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    ML352 was tested in Eurofin’s Lead Profiling Screen which is a binding assay panel of 68 GPCR’s, ion ...

    Potency
    Cellular
    In Vitro

    SLC5A7

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.bmcl.2015.02.058

    In Vivo Validations

    Rat
    Dose: 1 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 33 min
    Systemic clearance: 107 mL/min/kg
    Volume of Distribution at Steady-State: 3.2 L/Kg

    DOI Reference: 10.1016/j.bmcl.2016.08.062

    Mouse
    Dose: 1 mg/kg
    Route of delivery: Intraperitoneal
    Systemic clearance: 43.7mL/min/kg CL int and 29.4 mL/min/kg CL hep
    Target engagement assay: Plasma protein binding (Fu) 0.48

    DOI Reference: 10.1016/j.bmcl.2015.02.058

    Negative Control Compounds

    CANSAR1840627
    Notes: Cpd 2 IC50 4220 nM

    Chemical Information

    Molecular Formula C21H29N3O4
    SMILEs COc1ccc(C(=O)NCc2cc(C(C)C)no2)cc1OC1CCN(C)CC1
    InChI InChI=1S/C21H29N3O4/c1-14(2)18-12-17(28-23-18)13-22-21(25)15-5-6-19(26-4)20(11-15)27-16-7-9-24(3)10-8-16/h5-6,11-12,14,16H,7-10,13H2,1-4H3,(H,22,25)
    Molecular weight 387.22 Da
    AlogP 3.209600000000002
    HBond acceptors 7
    HBond donors 1
    Atoms 57

    References

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    Expert Reviews

    No SERP comments found for ML352

    Probe ML352 is in the process of SERP review.

    Please continue to check back for new reviews and commentary.