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FAH65E(-) | FAH65E(-) : Inhibitor of BACE1
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
BACE1
  • IC50:5 nM
  • EC50:EC50 ∼25 ​nM
  • % in:>90
Inhibitor
up to 500 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
FAH65 was found to be selective for BACE1 as the target enzyme. FAH65 did not significantly inhibite ...

Potency
Cellular
In Vitro

BACE1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.neurot.2025.e00610

In Vivo Validations

Mouse
Dose: 30 mg/Kg
Route of delivery: Oral
Cmax: 188 nM
Tmax: 1 h

Reference: --

Negative Control Compounds

canSAR7437552
Notes: Inactive enantiomer showing in vitro IC50>1000 uM

Chemical Information

Molecular Formula C22H19F2N5O2
SMILEs Cc1cc([C@]2(c3cccc(-c4cncnc4)c3)N=C(N)N(C)C2=O)ccc1OC(F)F
InChI InChI=1S/C22H19F2N5O2/c1-13-8-17(6-7-18(13)31-20(23)24)22(19(30)29(2)21(25)28-22)16-5-3-4-14(9-16)15-10-26-12-27-11-15/h3-12,20H,1-2H3,(H2,25,28)/t22-/m0/s1
Molecular weight 423.15 Da
AlogP 3.0837200000000005
HBond acceptors 7
HBond donors 2
Atoms 50

References

Publications

Cross References

Expert Reviews

by SERP
(on 31 Aug 2025 )
Cellular Use Rating
In Model Organisms
The compound should be best used up to 100 nM as at 1 µM some inhibition of BACE2 could be expected. It is also worth noting that the compound has only been tested in B254 mice overexpressing APP.
by SERP
(on 16 Sept 2025 )
Cellular Use Rating
In Model Organisms
To qualify as a probe with four stars the selectivity of FAH65E(-) needs to be shown versus a broader scope of biological targets.
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