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BRIVARACETAM | BRIVARACETAM : Inhibitor of SV2A
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
SV2A
  • Kd:540 nM
  • IC50:80 nM
  • Kd:62 nM
  • INH:3.2 µM
  • Kd:152 ± 40 nM
Inhibitor
1–10 μM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Brivaracetam was profiled at 10 μM (a concentration > 100 fold higher than its affinity for SV2A) ag ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Results from SV2A−/− knock-out mice clearly show that up to concentrations of 600 nm, [3H]BRV specif ...

Potency
Cellular
In Vitro

SV2A

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm030913e

In Vivo Validations

Rat
Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 1.7 h
Systemic clearance: 4.67 mL/min/kg
Tmax: 0.5 h
Bioavailability: ~100%

DOI Reference: 10.1021/jm030913e

Chemical Information

Molecular Formula C11H20N2O2
SMILEs CCC[C@@H]1CC(=O)N([C@@H](CC)C(N)=O)C1
InChI InChI=1S/C11H20N2O2/c1-3-5-8-6-10(14)13(7-8)9(4-2)11(12)15/h8-9H,3-7H2,1-2H3,(H2,12,15)/t8-,9+/m1/s1
Molecular weight 212.15 Da
AlogP 0.0
HBond acceptors 4
HBond donors 2
Atoms 35

References

Publications

Cross References

canSARChEMBLBindingDB

Expert Reviews

by SERP
(on 7 Aug 2024)
Cellular Use Rating
In Model Organisms
Matagne et al (2008) also dosed i.p. in various rat and mouse epilepsy models. Recommended dose would depend on the model but 10 mg/kg seems reasonable
by SERP
(on 24 Aug 2024)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
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