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PF-3845 | 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
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FAAH
  • Kinact, Ki:Kinact 3.3 nM
  • Ki:230 nM
  • IC50:18 nM
Covalent Inhibitor
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Selectivity Assessment Description:
Negligible activity against FAAH-2 (IC50>10 mM) in COS-7 cells. Profiled in vivo for FP-rhodam ...

Potency
Cellular
In Vitro

FAAH

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2009.02.013

In Vivo Validations

Mouse, Rat
Dose: 10 mg/Kg IP, 1-30 mg/Kg PO
Route of delivery: Oral, Intraperitoneal
Organ of interest (O): Brain

DOI Reference: 10.1016/j.chembiol.2009.02.013

Orthogonal Probes def

PF-04457845

Chemical Information

Molecular Formula C24H23F3N4O2
SMILEs O=C(Nc1cccnc1)N1CCC(Cc2cccc(Oc3ccc(C(F)(F)F)cn3)c2)CC1
InChI InChI=1S/C24H23F3N4O2/c25-24(26,27)19-6-7-22(29-15-19)33-21-5-1-3-18(14-21)13-17-8-11-31(12-9-17)23(32)30-20-4-2-10-28-16-20/h1-7,10,14-17H,8-9,11-13H2,(H,30,32)
Molecular weight 456.18 Da
AlogP 0.0
HBond acceptors 6
HBond donors 1
Atoms 56

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

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Expert Reviews

by SERP
(on 4 Jun 2021 )
Cellular Use Rating
In Model Organisms
There are two human FAAH enzymes (FAAH-1 and FAAH-2) that may collaborate to control Fatty Acid Amide catabolism. There is only a 20% sequence homology between the two enzymes and PF-3845 suffers from...
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