CG211 | CG211 : Inhibitor of RIOK2
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Control Compounds
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
RIOK2
  • Kd:6.1 ± 0.4 nM
  • IC50:139 ± 46 nM
  • ΔTm:~2 K
  • IC50:380 - 610 nM
  • INH:1 µM
Inhibitor
up to 5 µM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
KINOMEscan approach was used to test the specificity of the binding of compound CQ211 to RIOK2 by sc ...

Potency
Cellular
In Vitro

RIOK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.2c00271

In Vivo Validations

Rat
Dose:
Route of delivery: Intravenous
Plasma half life: 16.1 ± 1.9 h
Cmax: 586.8 ± 26.0 ng/mL
Tmax: 0.08 ± 0.00 h
Area Under the Curve:: 778.4 ± 29.8 h*ng/mL

DOI Reference: 10.1021/acs.jmedchem.2c00271

Dose:
Route of delivery: Oral
Plasma half life: 15.5 ± 10.8 h
Cmax: 13.1 ± 4.5 ng/mL
Tmax: 0.83 ± 1.01 h
Area Under the Curve:: 119.1 ± 17.0 h*ng/mL
Bioavailability: 3.1 ± 0.4%

DOI Reference: 10.1021/acs.jmedchem.2c00271

Mouse
Dose: 25 mg/kg
Route of delivery: Intraperitoneal

DOI Reference: 10.1021/acs.jmedchem.2c00271

Chemical Information

Molecular Formula C26H22F3N7O2
InChI InChI=1S/C26H22F3N7O2/c1-38-22-7-3-16(14-31-22)15-2-5-20-18(12-15)24-23(25(37)32-20)33-34-36(24)17-4-6-21(19(13-17)26(27,28)29)35-10-8-30-9-11-35/h2-7,12-14,30H,8-11H2,1H3,(H,32,37)
Molecular weight 521.18 Da
AlogP 0.0
HBond acceptors 9
HBond donors 2
Atoms 60
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

References

Cross References

canSARChEMBLBindingDBPDB

Expert Reviews


(on 3 Apr 2025 )
Cellular Use Rating
In Model Organisms
CQ211 shows adequate potency and selectivity and can be used as a probe in cells, with several reservations. 1) No cytotoxicity data is available in non-malignant cells, and 2) "CQ211 showed poor solubility...
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