GSK778

GSK778 : BD1 selective inhibitor of BRD2, BRD3, BRD4, BRDT

Structure

SERP Rating

Probe GSK778 is in the process of SERP review.

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Information

BRD2
BRD3
BRD4
BRDT

Inhibitor

up to 1 uM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: P25440

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 75 nM

Potency Assay: TR-FRET assay (BRD2 BD1)

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

Target aliases:

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

DOI Reference: 10.1021/acs.jmedchem.0c00566

Uniprot ID: P25440

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 13 nM

Potency Assay: BROMOScan (DiscoverX)

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

Target aliases:

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

DOI Reference: 10.1021/acs.jmedchem.0c00566

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: Excellent selectivity against other BRD-containing proteins (Bromoscan). Selectivity outside target family: Selectivity screen (50 targets tested): Closest hits are CHRNA1 (pIC50 = 6) and CYP3A4 (pIC50 = 6). Closest hits in the GPCR scan are DRD3 (Ki =485.92 nM), DRD4 (Ki =856.99 nM), GABAA (Ki =1595.89 nM) and GABAA/BZP (Ki = 1970.29 nM).

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SERP ratings and comments

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