GSK2830371

GSK2830371 : Allosteric inhibitor of Wip1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

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Probe GSK2830371 is in the process of SERP review.

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Information

PPM1D

Allosteric

up to 10 uM

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: O15297

Target Class: Enzyme

Target SubClass: Phosphatase

Potency: IC50

Potency Value: 6 nM

Potency Assay: FDP hydrolysis assay

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

Target aliases:

Protein phosphatase 1D, WIP1, PPM1D, PPM1D_HUMAN, ...

DOI Reference: 10.1038/nchembio.1427

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): GSK2830371 was tested for inhibition of biochemical activity against a panel of 21 phosphatases (Millipore PhosphataseProfiler): all IC50 >30000 nM.

Potency assay, off target (cells): Tested against various hematological cell lines

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Proteomic analysis (Silac) with GW2830371 and inactive analog 10 (same chemotype) in ref 10.1038/NCHEMBIO.1427 identified Wip1 as primary target.

(last updated: 21 Feb 2023 )