NUDT5-IN-9

NUDT5-IN-9 : Antagonist of NUDT5, NUDT14

Structure

SERP Rating

Probe NUDT5-IN-9 is in the process of SERP review.

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Information

NUDT5
NUDT14

Antagonist

up to 5 uM

In Vitro Validations

Uniprot ID: Q9UKK9

Target Class: Epigenetic

Target SubClass: Nudix

Potency: Kd

Potency Value: 237 nM

Potency Assay: SPR

PDB ID for probe-target interaction (3D structure): 8RIY

Target aliases:

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

DOI Reference: 10.1021/acs.jmedchem.4c00072

Uniprot ID: Q9UKK9

Target Class: Epigenetic

Target SubClass: Nudix

Potency: IC50

Potency Value: 270 nM

Potency Assay: Catalytic Assay (AMP-Glo)

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

Target aliases:

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

DOI Reference: 10.1021/acs.jmedchem.4c00072

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity of compound 9 as a NUDT5/NUDT14 inhibitor was confirmed by extended biophysical SPR screening of the NUDIX family.

Potency assay, off target (cells): Lower potency in binding to BTK in cells (EC50 = 0.377 ± 0.062 μM) with an approximately 75-fold decrease compared to the parent inhibitor ibrutinib.

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SERP ratings and comments

No SERP comments found for NUDT5-IN-9