Inverse agonist activity at human RORgammat assessed as inhibition of N-terminal biotinylated co-activator SRC1 recruitment measured after 60 mins by FRET assay
Inverse agonist activity at human RORgammat assessed as maximal inhibition of N-terminal biotinylated co-activator SRC1 recruitment measured after 60 mins by FRET assay relative to agonist
Inverse agonist activity at RORgammat in mouse CD4+ T cells assessed as inhibition of differentiation into Th17 cells by measuring IL-17 production at 0.3 uM by flow cytometry relative to control
Inverse agonist activity at human ROR-gammat LBD expressed in HEK293T cells assessed as inhibition of RORgammat transcription by Gal4-luciferase reporter assay
Protection against imiquimod-induced psoriasis in BALB/c mouse model assessed as reduction of skin scaling at 25 mg/kg, po dosed twice daily relative to control
Protection against imiquimod-induced psoriasis in BALB/c mouse model assessed as reduction in ear erythema at 25 mg/kg, po dosed twice daily relative to control
Protection against imiquimod-induced psoriasis in BALB/c mouse model assessed as reduction in back skin erythema at 25 mg/kg, po dosed twice daily relative to control