Table 2.

Inhibitory activity of benzene or naphthalene series with various fragments^a

^aInhibitory potency was estimated by both FP (used 100 nM Keap1 and 10 nM FITC-9mer Nrf2 peptide amide as a probe) and TR-FRET assays (used 5 nM Keap1 and 25 nM FITC-9mer Nrf2 peptide amide) that were performed in triplicates. 100 nM Keap1 and ND: not determined.

^bA is a phenyl ring scaffold and B is a naphthalene scaffold.

^cIC₅₀ is indicated as an average value of three replicates ± SEM (standard error of the mean).

^dK_i is calculated from the IC₅₀ values in FP or TR-FRET.