GSK2801

Antagonist of BAZ2A, BAZ2B

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(2 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

Protein target names: BAZ2A, BAZ2B

Mechanism of action: Antagonist

Primary References:

DOI - 10.1021/acs.jmedchem.5b00209

Probe Availability:

In Vitro Validations

Uniprot ID: Q9UIF9

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 257 nM

Potency Assay: Isothermal Titration Calorimetry and Biolayer interferometry

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

Structure-activity relationship: Yes

Target aliases:

Bromodomain adjacent to zinc finger domain protein ...

DOI Reference: 10.1021/acs.jmedchem.5b00209

Uniprot ID: Q9UIF9

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC 50

Potency Value: 400 nM

Potency Assay: Biochemical FRET assay

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

Target aliases:

Bromodomain adjacent to zinc finger domain protein ...

DOI Reference: 10.1021/acs.jmedchem.5b00209

In Cell Validations

In Vivo Data

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 10 Aug 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

GSK2801 PK parameters after IP/oral dosing in male CD1 mice suggest it has potential as in vivo probe, especially if applied side-by-side with structurally similar, negative control.

(last updated: 10 Aug 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

GSK2801 is a useful probe for BAZ2A and BAZ2B bromodomains. While it has encouraging selectivity relative to other bromodomains, the utility GSK2801 is somewhat limited by weak potency, requiring it to be employed at micromolar concentrations in cellular studies.

(last updated: 1 Feb 2017 )