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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

Vendors

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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 public 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