MS436

Inhibitor of BRD4, BRD3

Structure

SERP Rating

Probe MS436 is in the process of SERP review.

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Information

BRD4
BRD3

Inhibitor

up to 10 uM

Probe Availability:

In Vitro Validations

Uniprot ID: O60885

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Ki

Potency Value: 85 nM BD1; 340 nM BD2

Potency Assay: in vitro fluorescent anisotropy binding assay

PDB ID for probe-target interaction (3D structure): 4NUD

Structure-activity relationship: yes

Target aliases:

Bromodomain-containing protein 4, HUNK1, BRD4, BRD ...

DOI Reference: 10.1021/jm401334s

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): in vitro fluorescent anisotropy binding assay

Probe Selectivity in Vitro:

Selectivity against a panel of Bromodomains (Ki - uM): BRD4-BD2 0.34, BRD3-BD1 0.10, BRD3-BD2 0.14, related targets, BRD2 and BRDT were not tested, but are likely to bind MS436; CBP BrD 2.18, PCAF 5.52, BRD7 2.72, BPTF 6.06, BAZ2b 3.29, SMARCA4 7.97

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SERP ratings and comments

No SERP comments found for MS436