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GSK2801

Antagonist of BAZ2A, BAZ2B

Structure

Information

  • BAZ2A
  • BAZ2B
  • Antagonist

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

Off-Target Selectivity Assesments

Off Target: TAF1L
Potency end-point : IC 50 320 nM
Potency assay (off target): Thermal stability assays.
Probe Selectivity in Vitro:
42 Bromodomains tested, GSK2801 was only active against BRD9 1.1 uM and TAF1L 0.32 uM
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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 )