FIBOFLAPON

FIBOFLAPON : Inhibitor of ALOX5AP

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

ALOX5AP

Inhibitor

up to 100 nM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P20292

Target Class: Enzyme

Target SubClass: 5-lipoxygenase

Potency: IC50

Potency Value: 2.9 ± 1.0 nM

Potency Assay: FLAP binding assay (inhibition of 3H-ligand binding to FLAP membranes)

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

Target aliases:

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

DOI Reference: 10.1021/jm2008369

Uniprot ID: P20292

Target Class: Enzyme

Target SubClass: 5-lipoxygenase

Potency: IC50

Potency Value: 0.7 ± 03 nM

Potency Assay: Human Leukocyte Inhibition Assay (hLA)

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

Target aliases:

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

DOI Reference: 10.1021/jm2008369

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): AM803 had no COX-1 cross-reactivity and showed very little activity toward other enzymes in the leukotriene pathway (LTA4 hydrolase IC50 > 100 μM, LTC4 synthase IC50 = 36 μM, 5-LO IC50 = 20 μM) and no activity against the COX-2 enzyme (IC50 > 100 μM in a human blood assay measuring PGE2 inhibition). Inactivity against CYP3A4, CYP2C9 and CYP2D6. No inhibition of the CYP2C19, 2D6, and 1A2 enzymes.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 4 Nov 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Although Fiboflapon does not inhibit any of the major human CYP isoforms or the COX enzymes, wider profiling is lacking. There may thus be off-targets that limit the selectivity of the probe. The use of an orthogonal compound targeting FLAP/ALOX5AP is highly recommended.

(last updated: 23 Nov 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The compounds is an inhibitor of FLAP (5-lipoxygenase-activating protein) and thereby indirectly inhibits 5-LO. Synonyms: 936350-00-4, GSK2190915, AM-803, AM803

(last updated: 10 Dec 2023 )