BMS-986458

BMS-986458 : Degrader (PROTAC) of BCL6

Structure

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Information

BCL6

Degrader (PROTAC)

up to 100 nM

In Vitro Validations

Uniprot ID: P41182

Target Class: Transcription factor

Target SubClass: Transcriptional Repressor

Potency: IC50

Potency Value: 1.9 ± 0.8 nM

Potency Assay: Peptide displacement assay

PDB ID for probe-target interaction (3D structure): 9YA9

Target aliases:

B-cell lymphoma 6 protein, ZNF51, ZBTB27, LAZ3, BC ...

DOI Reference: 10.1021/acs.jmedchem.5c03123

Uniprot ID: P41182

Target Class: Transcription factor

Target SubClass: Transcriptional Repressor

Potency: IC50

Potency Value: 41 ± 12 nM

Potency Assay: CRBN binding assay

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

Target aliases:

B-cell lymphoma 6 protein, ZNF51, ZBTB27, LAZ3, BC ...

DOI Reference: 10.1021/acs.jmedchem.5c03123

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): In a panel of known CRBN neosubstrate assays, no degradation of CK1α, GSPT1, IKZF1, IZKF3, nor SALL4 was observed when testing BMS-986458 at concentrations up to 10 μM.

Potency assay, off target (cells): The selectivity of BMS-986458 was confirmed in a global proteomics study where BCL6 was the only significantly downregulated protein when OCI-LY-1 cells were treated with 100 nM BMS-984458 for 4 h and analyzed in comparison to DMSO-treated cells.

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