BI-5524

BI-5524 : Inhibitor of ELANE

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

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.

Information

ELANE

Inhibitor

up to 1 µM
Reviewer recommended concentration: a lower concentration around 5 nM could suffice

Probe Availability:

OpnMe

In Vitro Validations

Uniprot ID: P08246

Target Class: Enzyme

Target SubClass: peptidase S1 family

Potency: IC50

Potency Value: 0.5 nM

Potency Assay: hNE inhibitor assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Neutrophil elastase, ELA2, ELANE, ELNE_HUMAN, HLE, ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

BI-5524 displays a high selectivity for hNE (Inhibition of closely related proteases, like proteinase 3 and cathepsin G @ >100 nM and >10 µM, respectively). BI-5524 was also tested on 96 targets in a selectivity panel and showed ≥1,000-fold selectivity for all targets (≤ 50% inhibition @ 10 µM). BI-5525 was tested on 44 targets in a selectivity panel and showed ≥1,000-fold selectivity for all targets (≤ 50% inhibition @ 10 µM).

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

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 to interrogate inhibition of ELANE in mice and rats

(last updated: 17 May 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 20 May 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 5 Jun 2023 )