Chemical Probes logo
VU0361737 | VU0361737 : Positive Allosteric Modulator of GRM4
RATINGS:
Cellular Use: (3 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GRM4
    • EC50:240 nM
    Allosteric
    up to 10 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Within target family: tested against other members of the mGluR family with very little activity aga ...

    Potency
    Cellular
    In Vitro

    GRM4

    Mode of Action: Allosteric

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/jm9005065

    In Vivo Validations

    Rat
    Dose: 10 mg/Kg
    Route of delivery: Intraperitoneal
    Plasma half life: 1.9 (plasma), 0.15 (brain) h
    Systemic clearance: 895 (plasma) (mL/min)/kg
    Cmax: 154 (plasma), 1584 (brain) ng/mL
    Tmax: 0.5 (plasma, brain) h
    Area Under the Curve:: 173 (plasma), 705 (brain) ng·h/mL

    DOI Reference: 10.1021/jm9005065

    Chemical Information

    Molecular Formula C13H11ClN2O2
    SMILEs COc1cc(NC(=O)c2ccccn2)ccc1Cl
    InChI InChI=1S/C13H11ClN2O2/c1-18-12-8-9(5-6-10(12)14)16-13(17)11-4-2-3-7-15-11/h2-8H,1H3,(H,16,17)
    Molecular weight 262.05 Da
    AlogP 2.9959000000000007
    HBond acceptors 4
    HBond donors 1
    Atoms 29

    References

    Publications

    Cross References

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    Expert Reviews

    by SERP
    (on 18 Apr 2023 )
    Cellular Use Rating
    In Model Organisms
    Although VU0361737 has a decent cellular EC50 of 240 nM in a distal functional assay, the probe lacks any proof for a proximal interaction with the proposed target mGluR4. In addition, https://doi.org/10.1016/j.neuint.2020.104770...
    by SERP
    (on 19 Apr 2023 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP
    (on 7 May 2023 )
    Cellular Use Rating
    In Model Organisms
    Based on the data shared in (J. Med. Chem. 2009, 52, 4115–4118 4115 DOI: 10.1021/jm9005065), VU0361737 appears on the surface to be a useful cellular probe for mGluR4, particularyl considering its potency...
    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