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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

FAH65E(+)
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