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T-10418 | T-10418 : Agonist of GPR132
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GPR132
    • EC50:820 nM
    Agonist
    up to 10 µM based on EC50 and good selectivity profile
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    T-10418 was tested for GPCR selectivity in the PRESTO-Tango assay that measures association of a rec ...
    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Potential off-targets were tested using HEK293 cells stably express CMKLR1-eYFP or GPR1-eYFP treated ...

    Potency
    Cellular
    In Vitro

    GPR132

    Mode of Action: Agonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.3c02164

    In Vivo Validations

    Mouse
    Dose: 1 mg/Kg
    Route of delivery: Intravenous
    Systemic clearance: 16451 mL/(h·kg)
    Cmax: 45.3 ng/mL
    Tmax: 15 min
    Area Under the Curve:: 47.3 ng·h/mL

    DOI Reference: 10.1021/acs.jmedchem.3c02164

    Dose: 10 mg/Kg
    Route of delivery: Subcutaneous
    Systemic clearance: 8451 mL/(h·kg)
    Cmax: 755 ng/mL
    Tmax: 30 min
    Area Under the Curve:: 591 ng·h/mL

    DOI Reference: 10.1021/acs.jmedchem.3c02164

    Chemical Information

    Molecular Formula C22H20N2O4
    SMILEs O=C(N[C@H](Cc1ccccc1)C(=O)O)c1cccc(OCc2cccnc2)c1
    InChI InChI=1S/C22H20N2O4/c25-21(24-20(22(26)27)12-16-6-2-1-3-7-16)18-9-4-10-19(13-18)28-15-17-8-5-11-23-14-17/h1-11,13-14,20H,12,15H2,(H,24,25)(H,26,27)/t20-/m1/s1
    Molecular weight 376.14 Da
    AlogP 0.0
    HBond acceptors 6
    HBond donors 2
    Atoms 48

    Expert Reviews

    by SERP
    (on 30 Jul 2024 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP
    (on 31 Jul 2024 )
    Cellular Use Rating
    In Model Organisms
    While the agonistic potency, in vivo PK, and relevant data are not sufficient for routine use of this compound in investigating GPR132 biology/physiology, this compound could be considered the best option...
    by SERP
    (on 15 Aug 2024 )
    Cellular Use Rating
    In Model Organisms
    Due to its relatively weak potency this is not an ideal probe to study the biology of GPR132 in vitro, however there is limited choice for this target so it can be used with caution. The mouse PK data...
    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