GSK620

GSK620 : BD2 selective inhibitor of BRD2, BRD3, BRD4, BRDT

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe GSK620 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: 285 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.0c00796

Uniprot ID: P25440

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 318 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.0c00796

Uniprot ID: P25440

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 15 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.0c00796

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family - BROMOScan (DiscoverX) (34 tested): selective for the BD2 domain of BET proteins; closest hits: TAF1 BD2 (pKd = 5.4), EP300 (pKd = 5.1) and CREBBP (pKd = 5.0). Selectivity outside target family - Selectivity screen (48 targets tested): clean; Clean GPCR scan.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 15 Feb 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

GSK620 is a well-validated probe, coming from industrial experts in bromodomain-inhibitor design. This probe can be confidently used in both cellular and in vivo experiments as a pan-BET BD2 inhibitor.

(last updated: 25 Feb 2022 )