Table 1 Summary of compounds screened from commercial and in-house libraries and structure–activity relationship (SAR) analyses.
Library | Number screened | Primary screening (≥ 50% inhibition) | Hits confirmed (≥ 50% inhibition) | IC50 (< 10 µM) |
---|---|---|---|---|
In-house | 96 | 0 | – | – |
LOPAC-Pfizer | 90 | 1 | 0 | – |
Enzo-BML 2834 | 32 | 3 | 1 | 0 |
LOPAC-1280 | 1273 | 14 | 5 | 2 |
SAR | 12 | – | 4 | 1 |
Total | 1503 | 18 | 10 | 3 |