BI-665915

Inhibitor of ALOX5AP

Structure

SERP Rating

Probe BI-665915 is in the process of SERP review.

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Information

ALOX5AP

Inhibitor

30 – 500 nM, up to 2500 nM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P20292

Target Class: Membrane protein

Target SubClass: Five-Lipoxygenase Activating Protein

Potency: IC50

Potency Value: 1.7 nM

Potency Assay: FLAP binding assay

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

Target aliases:

Arachidonate 5-lipoxygenase-activating protein, AL ...

DOI Reference: 10.1021/jm501185j

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Extensive external screens: Invitrogen panel: 546 kinases < 30% inhibition @ 3µM; Panlabs External screen covering 68 targets: @ 10 µM; Cerep External screen covering 137 targets: @ 20 µM Closest off-target in the GPCR scan is SLC6A3 (60.66 % inhibition).

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