GSK046

GSK046 : BD2 selective inhibitor of BRD2, BRD3, BRD4, BRDT

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe GSK046 is in the process of SERP review.

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Information

BRD2
BRD3
BRD4
BRDT

Inhibitor

up to 10 uM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P25440

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 264 nM

Potency Assay: TR-FRET assay (BRD2 BD2)

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

Target aliases:

Bromodomain-containing protein 2, RING3, KIAA9001, ...

DOI Reference: 10.1021/acs.jmedchem.0c00605

Uniprot ID: P25440

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 250 nM

Potency Assay: BET mutant TR-FRET assay (BRD2 BD2)

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

Target aliases:

Bromodomain-containing protein 2, RING3, KIAA9001, ...

DOI Reference: 10.1021/acs.jmedchem.0c00605

Uniprot ID: P25440

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 35 nM

Potency Assay: BRD2 BD2 Bromoscan (DiscoverX)

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

Target aliases:

Bromodomain-containing protein 2, RING3, KIAA9001, ...

DOI Reference: 10.1021/acs.jmedchem.0c00605

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family - BROMOScan (DiscoverX) (40 tested): clean. Selectivity outside target family - Selectivity screen (48 targets tested): clean. Clean GPCR scan exept for one off-target: HTR1D Ki = 3438.75 nM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

GSK046 represents a valuable probe for the target family, with clean inhibition profile across a range of related and unrelated protein families. GSK046 is also suitable for in vivo studies, however given the constrained off-target testing, it should be used with a modicum of caution, however initial findings supports it use. The molecule is metabolically stable, with no obvious toxic profile. Overall, I am happy to recommend its use.

(last updated: 15 Feb 2022 )