BI-3802

Degrader of BCL6

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 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

Degrader

~~up to 1 uM~~
Reviewer recommended concentration: up to 5 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

PDB ID for probe-target interaction (3D structure): 5MW2, 6XMX

Structure-activity relationship: yes

Target aliases:

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

DOI Reference: 10.1016/j.celrep.2017.08.081

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Safety Screen 44 for GPCR and Invitrogen Kinase panel shows no inhibition, Whole-proteome quantification of SuDHL4Cas9 cells treated with 1 μM BI-3802 shows no other protein degradation.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 20 Mar 2021 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Limited oral bioavailability is noted following oral administration in SCID mice. Alternates routes are not explored.

(last updated: 29 Mar 2021 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This is an excellent chemical probe with a novel mechanism of action.

(last updated: 4 May 2021 )