MRK952

MRK952 : Inhibitor of NUDT5

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe MRK952 is in the process of SERP review.

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Information

NUDT5

Inhibitor

up to 1 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q9UKK9

Target Class: Epigenetic

Target SubClass: Nudix hydrolase

Potency: IC50

Potency Value: 85 nM

Potency Assay: AMP-GLO assay

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

Target aliases:

ADP-sugar pyrophosphatase, NUDIX5, NUDT5, NUDT5_HU ...

Other Reference: Peer reviewed at SGC

Uniprot ID: Q9UKK9

Target Class: Epigenetic

Target SubClass: Nudix hydrolase

Potency: Kd

Potency Value: 31 ± 18 nM

Potency Assay: SPR

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

Target aliases:

ADP-sugar pyrophosphatase, NUDIX5, NUDT5, NUDT5_HU ...

Other Reference: Peer reviewed at SGC

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity against the NUDT family was investigated via SPR with no hits.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

MRK-952 is a chemical probe for NUDT5. It binds the protein with an 31 nM IC50, whereas no binding was detected to a panel of 11 other NUDT family members. In a cellular assay, the compound inhibited NUDT5 binding to a nanoBRET probe at an EC50 of 24 nM. A closely related inactive control compound, MRK-952-NC, is available, that is >100-fold less active.

(last updated: 24 Jul 2023 )