GSK902056A

GSK902056A : Inhibitor of PKN3

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe GSK902056A is in the process of SERP review.

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Information

PKN3

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: Q6P5Z2

Target Class: Kinase

Target SubClass: AGC

Potency: Kd

Potency Value: 1 nM

Potency Assay: Kinobeads assay

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

Target aliases:

Serine/threonine-protein kinase N3, PKNBETA, PKN3, ...

DOI Reference: 10.1038/s41589-023-01459-3

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity was assessed over 278 Kinases using Kinobeads

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

The probe is potent and highly selective for PKN3 (Kinobeads Kd(app) = 1 nM, In-cell NanoBRET target engagement (TE) Kd(app) = 79 nM). Based on the nanoBRET TE data, the probe inhibits (binds) intracellular PKN3 to ~100% at 1 uM. Additional studies are needed to evaluate suitability for in vivo studies. Information about the probe's solubility, stability, and cytotoxicity have not been reported.

(last updated: 24 Feb 2025 )