T-690 | T-690 : Inhibitor of UGCG
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
UGCG
  • IC50:15 nM
  • EC50:4.4 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
SAFETYscan (DiscoverX (Eurofins) 47 targets at 10 µM): 44 target > 10 µM; HTR1B (EC50 = 1.5 μM), nAC ...

Potency
Cellular
In Vitro

UGCG

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.1c02078

In Vivo Validations

Mouse
Dose: 0.5 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.03 h (MRT)
Systemic clearance: 2022 mL/h/Kg
Volume of Distribution at Steady-State: 1974 L/Kg

DOI Reference: 10.1021/acs.jmedchem.1c02078

Dose: 5 mg/Kg
Route of delivery: Oral
Plasma half life: 1.91 h (MRT)
Cmax: 416 ng/mL
Area Under the Curve:: 829 ng*h/mL
Fb : 31%

DOI Reference: 10.1021/acs.jmedchem.1c02078

Chemical Information

Molecular Formula C22H20F3N3O4
SMILEs CC(C)(O)c1ccc(NC(=O)c2ccnn(-c3ccccc3OCC(F)(F)F)c2=O)cc1
InChI InChI=1S/C22H20F3N3O4/c1-21(2,31)14-7-9-15(10-8-14)27-19(29)16-11-12-26-28(20(16)30)17-5-3-4-6-18(17)32-13-22(23,24)25/h3-12,31H,13H2,1-2H3,(H,27,29)
Molecular weight 447.14 Da
AlogP 0.0
HBond acceptors 7
HBond donors 2
Atoms 52

References

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews


(on 19 Nov 2023 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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