NU227326

NU227326 : Inhibitor of IDO1

Structure

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Probe NU227326 is in the process of SERP review.

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Information

IDO1

Inhibitor

up to 100 nM, hook effect above this concentration

In Vitro Validations

Uniprot ID: P14902

Target Class: Enzyme

Target SubClass: Dioxygenase

Potency: Kd

Potency Value: 140 nM

Potency Assay: Biolayer interferometry (BLI) assay

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

Target aliases:

Indoleamine 2,3-dioxygenase 1, INDO, IDO, IDO1, I2 ...

DOI Reference: 10.1021/acs.jmedchem.5c00026

Uniprot ID: P14902

Target Class: Enzyme

Target SubClass: Dioxygenase

Potency: Kd

Potency Value: 321 nM

Potency Assay: Biolayer interferometry (BLI) assay of the ternary complex IDO1-PROTAC-CRBN

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

Target aliases:

Indoleamine 2,3-dioxygenase 1, INDO, IDO, IDO1, I2 ...

DOI Reference: 10.1021/acs.jmedchem.5c00026

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): To define the selectivity of the lead degrader and identify any other proteins that it degrade, NU227326 was tested in global quantitative proteomics at 1 μM for 24 h, in Kelly cells without induction by IFN-γ to assess unperturbed cells. Treatment with NU227326 only resulted in a significant decrease of 4–5 proteins (ADO, EPHX2, CDK8, and SALL4).

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