GNE-064

GNE-064 : Inhibitor of BRDs of SMARCA4, SMARCA2, PBRM1 (BD5)

Structure

SERP Rating

Probe GNE-064 is in the process of SERP review.

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Information

SMARCA4
SMARCA2
PBRM1

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: P51532

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 35 ± 1 nM

Potency Assay: TR-FRET

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

Target aliases:

Transcription activator BRG1, SNF2L4, SNF2B, BRG1, ...

DOI Reference: 10.1021/acs.jmedchem.2c00662

Uniprot ID: P51532

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 47 nM

Potency Assay: ITC

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

Target aliases:

Transcription activator BRG1, SNF2L4, SNF2B, BRG1, ...

DOI Reference: 10.1021/acs.jmedchem.2c00662

Uniprot ID: P51532

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 10 nM

Potency Assay: BromoSCAN

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

Target aliases:

Transcription activator BRG1, SNF2L4, SNF2B, BRG1, ...

DOI Reference: 10.1021/acs.jmedchem.2c00662

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): BromoSCAN of GNE-064 exhibit high potency against SMARCA2, SMARCA4, and PBRM1(5), modest affinity for PBRM1(2), and low micromolar affinity for BRD7 and BRD9. Compound 5 is ≥250-fold selective for SMARCA2, SMARCA4, and PBRM1(5) compared to all non-family VIII bromodomains.

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