Chemical Probes logo
PF-04457845 | Covalent Inhibitor of FAAH
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FAAH
  • IC50:7.2 nM (human), 7.4 nM (Rat)
  • IC50:3.2 nM
Covalent Inhibitor
40 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity profiling by competitive ABPP, shows no inhibition of ser. Hydrolases. Selectivity of ...

Potency
Cellular
In Vitro

FAAH

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? No

In Vivo Validations

Rat, Dog
Dose: 1 mg/Kg PO, 0.5 mg/Kg IV
Route of delivery: Intravenous, Oral
Plasma half life: 14.3 (R), 35.2 (D) h
Systemic clearance: 3.0 (R), 1.3 (D) mL/min/Kg
Organ of interest (O): Brain

Reference: --

Negative Control Compounds

PF-04875474

Orthogonal Probes def

PF-3845

Chemical Information

Molecular Formula C23H20F3N5O2
SMILEs O=C(Nc1cccnn1)N1CCC(=Cc2cccc(Oc3ccc(C(F)(F)F)cn3)c2)CC1
InChI InChI=1S/C23H20F3N5O2/c24-23(25,26)18-6-7-21(27-15-18)33-19-4-1-3-17(14-19)13-16-8-11-31(12-9-16)22(32)29-20-5-2-10-28-30-20/h1-7,10,13-15H,8-9,11-12H2,(H,29,30,32)
Molecular weight 455.16 Da
AlogP 0.0
HBond acceptors 7
HBond donors 1
Atoms 53

References

Publications

    Cross References

    canSARChEMBLBindingDBSGC Chemical Probes

    Vendors

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

    Expert Reviews

    by SERP
    (on 6 May 2021 )
    Cellular Use Rating
    In Model Organisms
    An excellent and very selective irreversible inhibitor of FAAH. Preincubation in vitro for 60 min is required to obtain maximum potency. Excellent brain penetration and efficacy with long duration of...
    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