Table 1.
GnRHR HTS campaign.
| Step | Screen type | Target | Number of compounds tested (5.2 μM) | Selection criteria | Number of selected compounds (hit rate) | Assay statistics | |
|---|---|---|---|---|---|---|---|
| Z′ | S/B | ||||||
| 1a | Primary screen | GNRHR | 646,275 | 11.40%a | 4,820 (0.75%) | 0.79 ± 0.06 | 2.46 ± 0.26 |
| 2a | Confirmation screen | GNRHR | 4,809 | 11.40%b | 1,668 (34.7%) | 0.76 ± 0.03 | 2.42 ± 0.04 |
| 2b | Confirmation screen (IPOne) | GNRHR | 4,809 | 21.87%c | 812 (16.9%) | 0.78 ± 0.02 | 1.72 ± 0.01 |
| 2c | Counterscreen screen | GNRHR + DOX | 4,809 | 41.6 %d | 32 (0.67%) | 0.81 ± 0.02 | 2.83 ± 0.05 |
| 3a | Dose response screen | GNRHR | 662 | EC50 < 5µM | 420 (63%) | 0.75 ± 0.03 | 2.32 ± 0.06 |
| 3b | Dose response screen (IPOne) | GNRHR | 662 | EC50 < 5µM | 466 (70%) | 0.79 ± 0.03 | 1.60 ± 0.02 |
| 3c | Dose response counterscreen | GNRHR + DOX | 662 | EC50 < 5µM | 0 (0%) | 0.77 ± 0.06 | 2.31 ± 0.21 |
| 4a | Powder confirmation (Fluo2) | GNRHR | 74 | EC50 < 5µM | 70 (95%) | 0.77 ± 0.034 | 1.65 ± 0.026 |
| 4b | Powder confirmation (Fluo2) | GNRHR + DOX | 74 | EC50 < 5µM | 0 (0%) | 0.66 ± 0.06 | 2.11 ± 0.02 |