Receptor-related orphan receptor γ (RORγ) has emerged as an attractive therapeutic target for the treatment of cancer and inflammatory diseases. XY123 potently inhibits the RORγ transcription activity with an IC₅₀ value of 64 nM. XY123 demonstrates good metabolic stability and a pharmacokinetics property with reasonable oral bioavailability (32.41%) and moderate half-life (4.98 h). 

All liver microsome assays were performed by Medicilon.

Reference:

Xishan Wu, et al. Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORγ Inverse Agonist. J Med Chem. 2021 Jun 24;64(12):8775-8797. doi: 10.1021/acs.jmedchem.1c00763.