Table 2. Antagonist potency (IC50), efficacy (% in parenthesis), and cell viability in qHTS.
| Compound Name (CAS No.) | Chemical Structure | Primary Screen Potency [μM] (Efficacy) | Follow-up Confirmation Potency [μM] (Efficacy) | Cytotoxicity* Potency [μM] (Efficacy) | Known modulator of CAR, CYP2B6, or CYP3A4? |
|---|---|---|---|---|---|
| Trifluridine (70-00-8) |  |
6.7 (-51%) | 4.5 (-73%) | Inactive | |
| Bosutinib (380843-75-4) |  |
0.67 (-61%) | 13.32 (-135%) | Inactive | |
| Ouabain (11018-89-6) |  |
0.30 (-104%) | 0.47 (-99%) | Inactive | |
| Digitoxin (71-63-6) |  |
0.08 (-76%) | 0.29 (-98%) | Inactive | |
| Nelfinavir (159989-64-7) |  |
9.52 (-88%) | 11 (-101%) | Inactive | |
| Adefovir (142340-99-6) |  |
0.76 (-102%) | 0.77 (-87%) | Inactive | CYP3A4 inhibitor |
| Mitomycin C (50-07-7) |  |
0.43 (-91%) | 0.75 (-110%) | Inactive | PXR deactivator |
| Topotecan (119413-54-6) |  |
0.06 (-94%) | 0.36 (-109%) | Inactive | |
| Daunorubicin (23541-50-6) |  |
0.60 (-87%) | 0.19 (-104%) | 15.9 (-43%) | |
| Bortezomib (179324-69-7) |  |
0.02 (-103%) | 0.03 (-101%) | 1.25 (-57%) |
*considered inactive if efficacy is less than 30%.