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BI-5524 | BI-5524 : Inhibitor of ELANE
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
ELANE
  • IC50:0.5 nM
  • EC50:0.4 nM
Inhibitor
a lower concentration around 5 nM could suffice
up to 1 µM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
BI-5524 displays a high selectivity for hNE (Inhibition of closely related proteases, like proteinas ...

Potency
Cellular
In Vitro

ELANE

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

In Vivo Validations

Mouse
Dose: 1 uM/Kg
Route of delivery: Intravenous
Plasma half life: 2.0 h
Systemic clearance: 19% QH
Cmax: 2280 nM (@ 10 uM/Kg
Tmax: 1.0 h
Bioavailability: 100%
Volume of Distribution at Steady-State: 2.0 L/Kg

Reference: --

Rat
Dose: 1 uM/Kg
Route of delivery: Intravenous
Plasma half life: 1.4 h
Systemic clearance: 52% QH
Cmax: 247596 (@196 uM/Kg
Tmax: 2.0 h
Bioavailability: 100%
Volume of Distribution at Steady-State: 3.1 L/Kg

Reference: --

Negative Control Compounds

CANSAR748058
Notes: in biochemical assay, BI-5525 shows IC50 >30 nM

Orthogonal Probes def

BAY-678

Chemical Information

Molecular Formula C26H23F3N4O4
SMILEs CC(C)(O)CNC(=O)N1C(=O)N(c2cccc(C(F)(F)F)c2)C2=C(C(=O)CC2)[C@H]1c1ccc(C#N)cc1
InChI InChI=1S/C26H23F3N4O4/c1-25(2,37)14-31-23(35)33-22(16-8-6-15(13-30)7-9-16)21-19(10-11-20(21)34)32(24(33)36)18-5-3-4-17(12-18)26(27,28)29/h3-9,12,22,37H,10-11,14H2,1-2H3,(H,31,35)/t22-/m1/s1
Molecular weight 512.17 Da
AlogP 4.65788
HBond acceptors 8
HBond donors 2
Atoms 60

Vendors

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Expert Reviews

by SERP
(on 17 May 2023 )
Cellular Use Rating
In Model Organisms
No data is provided for oral bioavailability (dosed by intravenous injection). IV exposure and elimination half-life are reasonable and thus BI-5524 and its enantiomer BI-5525 will be useful compounds...
by SERP
(on 20 May 2023 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 5 Jun 2023 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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