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GLPG0974 | Antagonist of FFAR2
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
FFAR2
    • IC50:9 nM
    • IC50:27-43 nM
    • IC50:483 nM
    Antagonist
    up to 100 nM

    Selectivity

    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    Within Target family: The close receptor homologue FFA3 (also called GPR41) is not inhibited by GLP ...

    Potency
    Cellular
    In Vitro

    FFAR2

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/jm5012885

    In Vivo Validations

    Rat
    Dose: 1 mg/Kg IV, 5-30 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Plasma half life: 1.7 h IV, 2.8 h PO 30 mg/Kg, 1.7 h PO 5 mg/Kg
    Systemic clearance: 2.1 L/h/Kg IV

    DOI Reference: 10.1021/jm5012885

    Orthogonal Probes def

    (S)-4-CMTB

    Chemical Information

    Molecular Formula C25H25ClN2O4S
    SMILEs C[C@]1(C(=O)N(CCCC(=O)O)Cc2cccc(Cl)c2)CCN1C(=O)c1csc2ccccc12
    InChI InChI=1S/C25H25ClN2O4S/c1-25(11-13-28(25)23(31)20-16-33-21-9-3-2-8-19(20)21)24(32)27(12-5-10-22(29)30)15-17-6-4-7-18(26)14-17/h2-4,6-9,14,16H,5,10-13,15H2,1H3,(H,29,30)/t25-/m1/s1
    Molecular weight 484.12 Da
    AlogP 0.0
    HBond acceptors 6
    HBond donors 1
    Atoms 58

    References

    Publications

    Cross References

    canSARChEMBLBindingDB

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    Expert Reviews

    by SERP
    (on 5 Aug 2021 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    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