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BI-3802 | BI-3802 : Molecular Glue of BCL6
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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, DC50, Dmax:20 nM DC50; 43 nM IC50; 80% Dmax
Molecular Glues
up to 5 uM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Safety Screen 44 for GPCR and Invitrogen Kinase panel shows no inhibition, Whole-proteome quantif ...

Potency
Cellular
In Vitro

BCL6

Mode of Action: Molecular Glues

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.celrep.2017.08.081

In Vivo Validations

Mouse
Dose: 10 mg/Kg, 100 mg/Kg
Route of delivery: Oral

DOI Reference: 10.1016/j.celrep.2017.08.081

Negative Control Compounds

BI-5273

Orthogonal Probes def

BI-3812

Chemical Information

Molecular Formula C24H29ClN6O3
SMILEs CNC(=O)COc1cc2cc(Nc3nc(N4C[C@@H](C)C[C@@H](C)C4)ncc3Cl)ccc2n(C)c1=O
InChI InChI=1S/C24H29ClN6O3/c1-14-7-15(2)12-31(11-14)24-27-10-18(25)22(29-24)28-17-5-6-19-16(8-17)9-20(23(33)30(19)4)34-13-21(32)26-3/h5-6,8-10,14-15H,7,11-13H2,1-4H3,(H,26,32)(H,27,28,29)/t14-,15+
Molecular weight 484.20 Da
AlogP 3.332600000000001
HBond acceptors 9
HBond donors 2
Atoms 63

References

Publications

Cross References

OpenMe

Vendors

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Expert Reviews

by SERP
(on 20 Mar 2021 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 29 Mar 2021 )
Cellular Use Rating
In Model Organisms
Limited oral bioavailability is noted following oral administration in SCID mice. Alternates routes are not explored.
by SERP
(on 4 May 2021 )
Cellular Use Rating
In Model Organisms
This is an excellent chemical probe with a novel mechanism of action.
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