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BI-3802

2D structure
Target BCL6 
Targeted domain BTB/POZ, binds at interface of 2 monomers
Mode of action Degrader
Control BI-5273
Orthogonal probe CCT369260  BI-3812  TP-021 
Recommended cellular usage concentration ≤ 1 µM
In vivo use No
Donated by Boehringer Ingelheim


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: IC50 ≤ 3 nM (BCL6:BCOR ULight TR-FRET; With affinities of approximately 3 nM, the assay wall of this assay is reached, limiting the accuracy.)
Selectivity within target family: > 30-fold Chemoaffinity pulldown with an immobilized BI-3802 analog: BCL6 was confirmed as the major target and no other BTB/POZ domain containing proteins were identified.
Selectivity outside target family Eurofins SafteyScreen (44 targets) at 10 µM [% ctrl]: with one hit HTR2B (agonist) (12% ctrl)
Invitrogen kinase panel (54 kinases) at 1µM with no hits <75% control
Clean PDSP scan (43 targets at 10 µM).
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: IC50 = 43 nM (BCL6::NCOR LUMIER in cells)
DC50 = 20 nM (BCL6 protein degradation in SU-DHL-4 cells)
Control compound (100 times less potent than the probe) BI-5273: IC50 = 10162 nM (BCL6::BCOR ULight TR-FRET); inactive in BCL6 protein degradation in SU-DHL-4 cells
Eurofins SafteyScreen (44 targets) at 10 µM: no hits <40% control