CPI-0610

CPI-0610 : BET family (BRD2, BRD4, BRD3, BRDT) inhibitor

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

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Information

BRD2
BRD4
BRD3
BRDT

Inhibitor

10-500 nM

Probe Availability:

MCULE

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.5b01882

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

CPI-0610 had IC50s>15 uM against other bromodomain proteins in Alphalisa assays (CBP, BRD9, BRPF1, PCAF, BRG1, ATAD2, TRIM24, and BRD8. CPI-0610 had no significant activity in Cerep panel of 50 GPCRs, ion channels and transporters or against common P450 enzyme isoforms at 10 uM.

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SERP ratings and comments

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 )