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BI-3812 | BI-3812 : PPI inhibitor of BCL6
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BCL6
  • IC50:≤ 3 nM
  • IC50:40 nM
PPI
Up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Safety Screen 44 for GPCR and Invitrogen Kinase panel shows no inhibition

Potency
Cellular
In Vitro

BCL6

Mode of Action: PPI

Structure-Activity-Relationship data available? No

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

Orthogonal Probes def

BI-3802

Chemical Information

Molecular Formula C26H32ClN7O5
SMILEs CNC(=O)COc1cc2cc(Nc3nc(N4CCC(C(=O)N(C)C)CC4)ncc3Cl)cc(OC)c2n(C)c1=O
InChI InChI=1S/C26H32ClN7O5/c1-28-21(35)14-39-20-11-16-10-17(12-19(38-5)22(16)33(4)25(20)37)30-23-18(27)13-29-26(31-23)34-8-6-15(7-9-34)24(36)32(2)3/h10-13,15H,6-9,14H2,1-5H3,(H,28,35)(H,29,30,31)
Molecular weight 557.22 Da
AlogP 0.0
HBond acceptors 12
HBond donors 2
Atoms 71

References

Publications

Cross References

canSARChEMBLBindingDBOpenMe

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Expert Reviews

by SERP
(on 29 Mar 2021 )
Cellular Use Rating
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.
by SERP
(on 10 Apr 2021 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 19 Apr 2021 )
Cellular Use Rating
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...
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. Read more about our evaluation criteria