NR1H2 and neoplasm: To overcomethe selectivity, Chen et al. screened 9500 in-house libraries usingmachine-learning-based virtual screening, which resulted in 59 biologicallyrelevant compounds with 13 LXRβ agonists.137 Further optimization efforts led to the identificationof the selective LXRβ agonist 285, which selectively binds toLXRβ (IC50 = 86 μM) and inhibits the growthof the U-87EGFRvIII cell line, with IC50 = 1.78 μM.Moreover, 285 displayed significant anti-tumor activityover the in vivo xenograft model and showed promisingPK properties (Figure 62E).