FMF-03-145-1

FMF-03-145-1 : Inhibitor of AURKA, AURKB, AURKC

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 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

AURKA
AURKB
AURKC

Inhibitor

up to 1 uM

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: O14965

Target Class: Kinase

Target SubClass: Ser/Thr kinase

Potency: IC50

Potency Value: 52 nM

Potency Assay: Z’LYTE kinase assay

PDB ID for probe-target interaction (3D structure): 5ONE

Target aliases:

Aurora kinase A, STK6, STK15, IAK1, BTAK, AYK1, AU ...

DOI Reference: 10.1016/j.bmcl.2017.08.016

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Off Target: PLK4

Potency end-point : IC50 82 nM

Potency assay (off target): Exclusively on-target activity detected by KINOMEscan ® at 1 μ M compound concentration with only one off-target identified (PLK4).

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

An orthogonal PLK4 inhibitor should be used in parallel to rule out phenotypic effects that result from PLK4 inhibition.

(last updated: 23 Dec 2022 )

SERP Ratings

In Cell Rating

SERP Comments:

A great addition to known AURK inhibitors and worth using in cells for this family of kinases. With several AURK probes and inhibitors available, this should be used in combination with other structurally differentiated compounds.

(last updated: 3 Jan 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Considering that FMF-03-145-1 addresses the off-target PLK4 with an in vitro IC50 of 82 nM, which is comparable to the IC50 of the aurora kinases, an additional AURK probe with a different selectivity profile (no PLK4 inhibition) is necessary in cellular assays to ensure that cellular effects are not wrongfully attributed to AURK inhibition.

(last updated: 22 Mar 2023 )