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BMS-820132 | BMS-820132 : Partial Activator of GCK
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
GCK
  • Activity:29 nM; max activation 143%
    Partial Activator
    Based on the reported chronic experiment, repeated dosing of 30 mg/kg daily was safe and efficacious in mouse and would be the in vivo dose I'd recommend in mouse.
    1 µM

    Selectivity

    Potency
    Cellular
    In Vitro

    GCK

    Mode of Action: Partial Activator

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.1c02110

    In Vivo Validations

    Mouse
    Dose: 2.5 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 2.1 h
    Systemic clearance: 2.9 mL/min/kg
    Area Under the Curve:: 24.9 uM*h
    Volume of Distribution at Steady-State: 0.3 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.1c02110

    Dose: 5 mg/Kg
    Route of delivery: Oral
    Cmax: 14.1 uM
    Tmax: 0.5 h
    Area Under the Curve:: 49.7 uM*h
    Bioavailability: 100%

    DOI Reference: 10.1021/acs.jmedchem.1c02110

    Rat
    Dose: 2.5 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 0.9 h
    Systemic clearance: 4.4 mL/min/kg
    Area Under the Curve:: 16.6 uM*h
    Volume of Distribution at Steady-State: 0.3 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.1c02110

    Dose: 5 mg/Kg
    Route of delivery: Oral
    Cmax: 13.0 uM
    Tmax: 0.9 h
    Area Under the Curve:: 29.5 uM*h
    Bioavailability: 90%

    DOI Reference: 10.1021/acs.jmedchem.1c02110

    Dog
    Dose: 3 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 1.8 h
    Systemic clearance: 7.2 mL/min/Kg
    Area Under the Curve:: 12.3 uM*h
    Volume of Distribution at Steady-State: 0.5 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.1c02110

    Dose: 3 mg/Kg
    Route of delivery: Oral
    Cmax: 4.9 uM
    Tmax: 0.8 h
    Area Under the Curve:: 8.0 uM*h
    Bioavailability: 66%

    DOI Reference: 10.1021/acs.jmedchem.1c02110

    Monkey (Cynomolgus)
    Dose: 3 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 1.9 h
    Systemic clearance: 22.7 mL/min/Kg
    Area Under the Curve:: 3.8 uM*h
    Volume of Distribution at Steady-State: 1.1 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.1c02110

    Dose: 3 mg/Kg
    Route of delivery: Oral
    Cmax: 0.38 uM
    Tmax: 1.3 h
    Area Under the Curve:: 0.57 uM*h
    Bioavailability: 15%

    DOI Reference: 10.1021/acs.jmedchem.1c02110

    Chemical Information

    Molecular Formula C26H33N6O7P
    SMILEs CCOP(=O)(Cn1ccc(NC(=O)c2cc(Oc3cnc(C(=O)N4CCC4)cn3)cc(OC(C)C)c2)n1)OCC
    InChI InChI=1S/C26H33N6O7P/c1-5-36-40(35,37-6-2)17-32-11-8-23(30-32)29-25(33)19-12-20(38-18(3)4)14-21(13-19)39-24-16-27-22(15-28-24)26(34)31-9-7-10-31/h8,11-16,18H,5-7,9-10,17H2,1-4H3,(H,29,30,33)
    Molecular weight 572.21 Da
    AlogP 0.0
    HBond acceptors 13
    HBond donors 1
    Atoms 73

    References

    Publications

    Cross References

    canSARChEMBLBindingDBPDB

    Vendors

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    Expert Reviews

    by SERP
    (on 22 Dec 2022 )
    Cellular Use Rating
    In Model Organisms
    Activity in biochemical assay but no cellular data was reported for the compound. It should be mentioned that While the PK data are reported for mouse, rat, dog and cyno, the biochemical activity was reported...
    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