GSK6853

GSK6853 : Inhibitor of BRPF1

Structure

SERP Rating

Probe GSK6853 is in the process of SERP review.

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Information

BRPF1

Inhibitor

up to 1 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P55201

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 7.9 nM

Potency Assay: TR-FRET

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

Target aliases:

Peregrin, BR140, BRPF1, BRPF1_HUMAN, Protein Br140 ...

DOI Reference: 10.1021/acsmedchemlett.6b00092

Uniprot ID: P55201

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 0.31 nM

Potency Assay: BromoSCAN

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

Target aliases:

Peregrin, BR140, BRPF1, BRPF1_HUMAN, Protein Br140 ...

DOI Reference: 10.1021/acsmedchemlett.6b00092

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Within target family: BromoSCAN against 34 DNA-tagged bromodomains, greater than 1600-fold selectivity over all other bromodomains tested Outside target family: Tested activity in 48 unrelated assays.

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SERP ratings and comments

No SERP comments found for GSK6853

Portal Comments

In a 2023 study, Hu et al. evaluated GSK6853 in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations near 1 uM. (DOI:10.1016/j.chembiol.2023.09.003)

(last updated: 7 Nov 2023)