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- W2943964900 abstract "A high-throughput screen against Inventiva’s compound library using a Gal4/RORγ-LBD luciferase reporter gene assay led to the discovery of a new series of quinoline sulphonamides as RORγ inhibitors, eventually giving rise to a lead compound having an interesting in vivo profile after oral administration. This lead was evaluated in a target engagement model in mouse, where it reduced IL-17 cytokine production after immune challenge. It also proved to be active in a multiple sclerosis model (EAE) where it reduced the disease score. The synthesis, structure activity relationship (SAR) and biological activity of these derivatives is described herein." @default.
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- W2943964900 date "2019-07-01" @default.
- W2943964900 modified "2023-10-01" @default.
- W2943964900 title "Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists" @default.
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- W2943964900 doi "https://doi.org/10.1016/j.bmcl.2019.05.015" @default.
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