Vimirogant

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency: 

IC50

3.7 nM

Potency assay: 

radio-ligand RORγ binding scintillation proximity assay

PDB ID for probe-target interaction (3D structure): 

5NTW

Structure-activity relationship: 

yes

Off target activity

Probe Selectivity in Vitro: 

more than 1000-fold selectivity against other ROR isoforms

In cell validation

On target activity in cells

Potency in cells: 

IC50

17 nM

Off target activity in cells

Probe Selectivity in Cell: 

inhibit hERG by 45.4% at 3 μM

In vivo validation

Organism: 

Mouse, Rat, Dog

Dose: 

15-100 mg/Kg

Route of delivery: 

Oral

Plasma half life: 

6 (R), 15 (D) h

Bioavailability: 

64 (R), 66 (D) %