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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

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 public 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