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VU6081679 | VU6081679 : Positive Allosteric of GRM8
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
GRM8
    • EC50:162 nM
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Selectivity within target family: selective over the other two widely CNS expressed Group III mGlus, ...
    Selectivity Assessment Description:
    Eurofins Lead Profiling Screen Radioligand binding panel of 44 targets including GPCRs, ion channel ...

    Potency
    Cellular
    In Vitro

    GRM8

    Mode of Action: Positive Allosteric

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acschemneuro.6c00364

    In Vivo Validations

    Rat
    Dose: 1 mg/Kg IV, 10 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Plasma half life: 0.91 h
    Systemic clearance: 22.4 mL/min/kg
    Bioavailability: 102%
    Volume of Distribution at Steady-State: 1.38 L/Kg
    Target engagement assay: Kp brain/plasma 0.16, Kp,uu brain/plasma 0.19

    DOI Reference: 10.1021/acschemneuro.6c00364

    Chemical Information

    Molecular Formula C22H20FN5O3
    SMILEs COc1ccc(-c2ccc(=O)n(Cc3cnc(-c4cnn(C)c4)c(F)c3)n2)cc1OC
    InChI InChI=1S/C22H20FN5O3/c1-27-13-16(11-25-27)22-17(23)8-14(10-24-22)12-28-21(29)7-5-18(26-28)15-4-6-19(30-2)20(9-15)31-3/h4-11,13H,12H2,1-3H3
    Molecular weight 421.16 Da
    AlogP 2.910400000000001
    HBond acceptors 8
    HBond donors --
    Atoms 51

    References

    Publications

    Cross References

    canSAR: 7719235 PubChem: 179075708

    Expert Reviews

    by SERP
    (on 26 Sept 2026)
    Cellular Use Rating
    In Model Organisms
    VU6081679 is a very useful and well-characterized tool to study mGlu8. It shows good, consistent activity across mouse, rat, and human receptors, which makes it easy to compare findings between cells and...
    by SERP
    (on 16 Oct 2026)
    Cellular Use Rating
    In Model Organisms
    VU6081679 is a CNS-penetrant pyridazinone mGlu8 PAM with reasonable, species-consistent cellular potency, a clean ancillary pharmacology panel, and no CYP450 inhibition (IC50 > 30 µM for 1A2/2C9/2D6/3A4)....
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