Table 1. Screening results, including compound totals for each library.
Bioactives | GHCDL | |
---|---|---|
Total compounds | 10,453 | 68,489 |
Hits (≥ 70% inhibition) | 734 | 78 |
Raw hit rate (%) | 7.02 | 0.11 |
Cytotoxicity filter | 130 | N/A |
Filtered hit rate (%) | 1.24 | 0.11 |
Reconfirmed hits | 75 | 31 |
Reconfirmation rate (%) | 57.7 | 39.7 |
EC50 ≤ 1 μM | 49 | 18 |
Selected filtered hits (CC50:EC50 ≥ 10) | 10 | 2 |
A host cell cytotoxicity filter was applied (≥ 40% HCT-8 cell inhibition) and the remaining compounds were tested in triplicate for reconfirmation. Reconfirmed hits were then tested in dose-response, and compounds were further filtered by potency and selectivity (final row).