Table 1. SAR Studies around the C-4 Isoxazole Positiona.

cLogP values, glide scores, TR-FRET IC50 values (μM) from coactivator recruitment and AlexaFluor-MRL-871 displacement assays, ΔTm values (°C) from thermal shift assays, and fold decrease in IL-17a mRNA expression levels relative to DMSO reverse transcriptase PCR (RT-PCR). Abbreviations: n.d., not determined. TR-FRET and TSA data are recorded in triplicate; values are representative of ≥3 repeated experiments. RT-PCR data are recorded in triplicate; values are representative of ≥2 repeated experiments. cLogP values were predicted using MarvinSketch (20.10).
