AZD5305

AZD5305 : Inhibitor of PARP1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe AZD5305 is in the process of SERP review.

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Information

PARP1

Inhibitor

100 nM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P09874

Target Class: Other post-translational modification

Target SubClass: PARP

Potency: IC50

Potency Value: 3 nM

Potency Assay: PARP Fluorescence Anisotropy Binding Assays

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

Target aliases:

Poly [ADP-ribose] polymerase 1, PPOL, ADPRT, PARP1 ...

DOI Reference: 10.1021/acs.jmedchem.1c01012

Uniprot ID: P09874

Target Class: Other post-translational modification

Target SubClass: PARP

Potency: Ki

Potency Value: 0.13 nM

Potency Assay: Total Internal Fluorescence (TIRF) microscopy

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

Target aliases:

Poly [ADP-ribose] polymerase 1, PPOL, ADPRT, PARP1 ...

DOI Reference: 10.1021/acs.jmedchem.1c01012

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

PARP Family Proteomic Data demonstrate that AZD5305 is highly selective for PARP1 over the other members of the PARP family. TIRF microscopy revealed a pKi of 3.3 µM for PARP2.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

AZD5305 is one of the most PARP1 potent and selective inhibitors against other PARPs with high physicochemical and DMPK profiles, so it should be the great compound to evalutate PARP1 biology.

(last updated: 1 May 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

AZD5305 is a highly potent PARP1 inhibitor that functions through the PARP-DNA trapping mechanism. It is highly selective against PARP2, exhibiting cytotoxic effects in a PARP1-dependent and PARP2-independent manner in BRCA2-null cells. This is an outstanding compound to probe PARP1 versus PARP2 function.

(last updated: 15 May 2023 )