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OL-135 | OL-135 : Inhibitor of FAAH2
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FAAH2
  • Ki:4.7 nM
  • IC50:13.4 nM
  • EC50:450 nM
FAAH
  • IC50:206 nM
    Inhibitor
    up to 10 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    Selectivity was assessed against KIAA and TGH with IC50 >100 and 0.6 uM. Also in proteomics analysis ...

    Potency
    Cellular
    In Vitro

    FAAH2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/jm049614v

    FAAH

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1074/jbc.M606646200

    In Vivo Validations

    Mouse
    Dose: 10 mg/Kg
    Route of delivery: Intraperitoneal

    DOI Reference: 10.1124/jpet.104.069401

    Orthogonal Probes def

    PF-04457845

    Chemical Information

    Molecular Formula C21H22N2O2
    SMILEs O=C(CCCCCCc1ccccc1)c1ncc(-c2ccccn2)o1
    InChI InChI=1S/C21H22N2O2/c24-19(14-7-2-1-4-10-17-11-5-3-6-12-17)21-23-16-20(25-21)18-13-8-9-15-22-18/h3,5-6,8-9,11-13,15-16H,1-2,4,7,10,14H2
    Molecular weight 334.17 Da
    AlogP 5.112500000000005
    HBond acceptors 4
    HBond donors --
    Atoms 47

    References

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    Expert Reviews

    by SERP
    (on 29 Aug 2022 )
    Cellular Use Rating
    OL-135 displayed inhibitory activity against recombinant human Fatty-acid amide hydrolase (FAAH) in cell-free assays at low nanomolar concentrations. In T84 cells, it showed inhibitory activity against...
    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