CPI-0610

Antagonist, Reversible, competitive inhibitor of BRD2, BRD4, BRD3, BRDT

Structure

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In Cells

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In Model Organisms

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Information

Protein target names: BRD2, BRD4, BRD3, BRDT

Mechanism of action: Antagonist, Reversible, competitive inhibitor

Recommended in-cell concentration:

10-500 nM

Primary References:

Probe Availability:

Cayman (1380087-89-7)

In Vitro Validations

Uniprot ID: P25440

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 160 nM BD1, 25 nM BD2

Potency Assay: Alphalisa assay

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

Structure-activity relationship: Yes, see J Med Chem paper

Target aliases:

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

DOI Reference: 10.1021/acs.jmedchem.5b0188

In Cell Validations

In Vivo Data

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SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 19 May 2017 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 22 May 2017 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 13 Jul 2017 )