BAY-707

Inhibitor of NUDT1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(1 ratings)

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Probe BAY-707 is in the process of SERP review.

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Information

NUDT1

Inhibitor

1 nM to 1 µM

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Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P36639

Target Class: Epigenetic

Target SubClass: Nudix Hydrolase

Potency: IC50

Potency Value: 2.3 nM

Potency Assay: MTH1 enzymatic assay

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

Structure-activity relationship: Yes

Target aliases:

Oxidized purine nucleoside triphosphate hydrolase, ...

DOI Reference: 10.1021/acschembio.7b00370

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Tm shift assay

Probe Selectivity in Vitro:

BAY-707 is a selective NUDT1 (MTH1) inhibitor across the Nudix family

Probe Selectivity in Cell:

high selectivity in an in-house kinase panel comprised of 30 kinases

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

BAY-707 is a potent inhibitor of the NUTD1 (MHT1) hydrolase. It was selective across the Nudix family. However, additional selectivity data outside the Nudix family has not been published. Therefore, some caution should be used in interpreting phenotypic data. BAY-707 has been used in vivo, although only very limited dosing and pharmacokinetic data have been published.

(last updated: 28 Jun 2020 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

BAY-707 is a potent, selective NUDT1 inhibitor that demonstrates enzymatic inhibition in vitro, and cellular target engagement in cells using CETSA. It does not demonstrate broad anti-cancer activity in cells nor activity in 2 in vivo mouse xenograft models (100 mg/kg oral dose). Double-stranded DNA breaks with compounds from this series are unlikely to result from direct target engagement. BAY-707 shows no effect on nuclear 8-oxo-dG levels.

(last updated: 7 Sept 2021 )