AZD5153

AZD5153 : Bivalent inhibitor of BD1-BD2 of BRD4, BRD2, BRDT, BRD3

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe AZD5153 is in the process of SERP review.

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Information

BRD4
BRD2
BRDT
BRD3

Bivalent BD1-BD2

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: O60885

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Ki

Potency Value: 5 nM

Potency Assay: BRD4 Fluorescence Polarization Assay

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

Target aliases:

Bromodomain-containing protein 4, HUNK1, BRD4, BRD ...

DOI Reference: 10.1021/acs.jmedchem.6b00070

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): AZD5153 (10 μM) was tested for activity across 32 bromodomains in the Bromoscan panel showing inherent selectivity for the BET family isolated bromodomains; the next most potent BRD was TAF1(2) (pKi 5.9).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

AZD5153 is a high quality compound that has progressed to the clinical trial stage. The compound binds both bromodomains of the BET family members (BRD4 , BRD2, BRD3, BRDT) with comparable affinities, and at least an order of magnitude more potently compared to other bromodomains. Its optimized pharmacological properties make it suitable for in vivo studies. AZD5153, therefore, is a good choice for a pan-BET inhibitor that complements additional available chemical tools with different mechanisms (selectivity, degradation) to target this widely studied protein family.

(last updated: 17 Apr 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

AZD5153 is a potent and well characterized BET inhibitor that binds both Bromo domains of BET proteins. Its comprehensive characterization makes it a great tool for studying the BET protein function in cells and in vivo.

(last updated: 24 Apr 2023 )