CCT374705 | CCT374705 : Inhibitor of BCL6
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BCL6
  • IC50:6 nM
  • IC50:22 nM
  • GI50:14.9 - 1850 nM
Inhibitor
up to 1 µM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Safety profiling of CCT374705 was carried out, and all targets (78) showed a Kd above 1 μM, although ...

Potency
Cellular
In Vitro

BCL6

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.3c00155

In Vivo Validations

Mouse
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 2.94 h IV
Systemic clearance: 1.6 mL/min/Kg IV
Cmax: 8652 nM PO
Area Under the Curve:: 42883 nM*h PO
Fb : 99.283%
Bioavailability: 48% PO
Volume of Distribution at Steady-State: 0.39 L IV

DOI Reference: 10.1021/acs.jmedchem.3c00155

Chemical Information

Molecular Formula C21H18ClF3N4O2
SMILEs Cn1c(=O)c2c(c3cc(Nc4ccnc(F)c4Cl)ccc31)N[C@@H](C1CC1)C(F)(F)CO2
InChI InChI=1S/C21H18ClF3N4O2/c1-29-14-5-4-11(27-13-6-7-26-19(23)15(13)22)8-12(14)16-17(20(29)30)31-9-21(24,25)18(28-16)10-2-3-10/h4-8,10,18,28H,2-3,9H2,1H3,(H,26,27)/t18-/m0/s1
Molecular weight 450.11 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 49

References

Cross References

canSARPDB

Vendors

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Expert Reviews


No SERP comments found for CCT374705

Probe CCT374705 is in the process of SERP review.

Please continue to check back for new reviews and commentary.