CCT373566 | CCT373566 : Molecular Glue for BCL6
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BCL6
  • IC50:2.2 nM
  • DC50:0.7 nM
  • DC50:1.0 nM
  • GI50:1.4 - 12.5 nM
Molecular Glues
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity profiling of CCT373566 against kinases (468) and a safety panel (78) at 1 μM confirmed s ...

Potency
Cellular
In Vitro

BCL6

Mode of Action: Molecular Glues

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.1c02175

In Vivo Validations

Mouse
Dose: 1 mg/kg IV, 5 mg/kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 1.15 h
Systemic clearance: 5.7 mL/min/Kg (6% Qh)
Cmax: 3947 nM/L
Fb : 99.88%
Bioavailability: 44%
Volume of Distribution at Steady-State: 0.47 L/Kg

DOI Reference: 10.1021/acs.jmedchem.1c02175

Negative Control Compounds

canSAR3997277
Notes: Negative control CCT373567 shows a DC50 >2000 in MSD degradation assay

Chemical Information

Molecular Formula C26H29ClF2N6O3
InChI InChI=1S/C26H29ClF2N6O3/c1-13-7-16(36)11-35(10-13)25-30-9-18(27)23(33-25)31-15-5-6-19-17(8-15)20-21(24(37)34(19)2)38-12-26(28,29)22(32-20)14-3-4-14/h5-6,8-9,13-14,16,22,32,36H,3-4,7,10-12H2,1-2H3,(H,30,31,33)/t13-,16+,22-/m0/s1
Molecular weight 546.20 Da
AlogP 0.0
HBond acceptors 9
HBond donors 3
Atoms 67

References

Cross References

canSARChEMBLBindingDBPDB

Expert Reviews


No SERP comments found for CCT373566

Probe CCT373566 is in the process of SERP review.

Please continue to check back for new reviews and commentary.