AZD-4017

AZD-4017 : Inhibitor of HSD11B1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe AZD-4017 is in the process of SERP review.

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Information

HSD11B1

Inhibitor

up to 100 nM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P28845

Target Class: Enzyme

Target SubClass: Dehydrogenase

Potency: IC50

Potency Value: 7 nM

Potency Assay: cortisol competitive homogeneous time-resolved fluorescence assay (HTRF) assay

PDB ID for probe-target interaction (3D structure): 4HFR

Target aliases:

11-beta-hydroxysteroid dehydrogenase 1, SDR26C1, H ...

DOI Reference: 10.1021/jm300592r

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): AZD-4017 displayed excellent selectivity versus the related enzymes 11-βHSD2, 17β-HSD1, 17β-HSD3 (all IC50 > 30 μM) and showed no measurable activity against the glucocorticoid and mineralocorticoid receptors. Outside target family: A good selectivity profile was observed versus a panel of 119 unrelated enzymes and receptors, with the only two weak hits being angiotensin (AT2) receptor and choleocystokinin (CCK2) receptor.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

While potent against human 11β-HSD1, the inhibitor is much less potent against mouse, rat, or dog orthologs. Therefore, use of this compound is supported in human cell lines expressing 11β-HSD1; it is NOT recommended for use in mouse, rat, or dog cell lines.

(last updated: 4 Oct 2023 )