BI-3812

BI-3812 : PPI inhibitor of BCL6

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

BCL6

Up to 1 uM

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Probe Availability:

In Vitro Validations

Uniprot ID: P41182

Target Class: Transcription factor

Target SubClass: Transcriptional Repressor

Potency: IC50

Potency Value: ≤ 3 nM

Potency Assay: BCL6::BCOR ULight TR-FRET assay.

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

Structure-activity relationship: yes

Target aliases:

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

DOI Reference: 10.1038/s41586-020-2925-1

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Safety Screen 44 for GPCR and Invitrogen Kinase panel shows no inhibition

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

While validated as an inhibitor of BCL6 for use in cells (at 1 µM), chemically induced BCL6 degraders have stronger effects than BCL6 inhibition using this compound.

(last updated: 29 Mar 2021 )

SERP Ratings

In Cell Rating

(last updated: 10 Apr 2021 )

SERP Ratings

In Cell Rating

SERP Comments:

This is a potentially very interesting molecule, but its putative and relatively complex mechanism of action (binder/degrader whose activity depends also on other domains not directly targeted) makes it still not ideal as bona fide validated chemical probe. The authors also do not recommend using this probe in vivo (10.1016/j.celrep.2017.08.081, albeit only a limited oral PK was performed). Investigators are recommended to carefully read the original manuscripts reported above prior to use this agent and carefully evaluate and interpret their results in the context of these previous findings.

(last updated: 19 Apr 2021 )