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Trypanosome cell, human (MRC5) cell, and pooled human microsomal intrinsic clearance (Cli) data for key (representative) compounds from series 1–3.
| Compd | Series | TbTryS IC50 [μm] | Tb EC50 [μm] | MRC5 EC50 [μm] | Cli [mL min−1 g−1] |
|---|---|---|---|---|---|
| 8 | 1 a | 0.41 | 22 | >50 | 0.9 |
| 26 | 1 c | 14 | 14 | >50 | 3.0 |
| 36 | 2 a | 8.5 | 32 | >50 | 9.1 |
| 57 | 2 c | 2.4 | 19 | >50 | 17 |
| 71 | 3 | 0.09 | 7.9 | >50 | 1.6 |
| 84 | 3 | 0.045 | 5.4 | 20 | ND[a] |
| 89 | 3 | 0.14 | 5.1 | >50 | ND[a] |
[a] Not determined.
