Table 2.
Assay activity summary of the nine hit clusters identified from the L. donovani and T. cruzi screen campaign. “Active compounds” are those with AmMac or AmCel pIC50 > 5 and only selective compounds were considered (Mac or H9c2 pIC50 < 5).
| Cluster ID | Compounds tested |
L. donovani |
T. cruzi |
|||
|---|---|---|---|---|---|---|
| Number of active compounds | InMac assay pIC50 range | Number of active compounds | Imaging assay pIC50 range | Trypomastigotes assay 72 h pIC50 range | ||
| A | 15 | 2 | AmMac 5.06–6.30 InfCel 4.91–6.27 Mac <4.3 |
6 | AmCel 5.05–5.85 InfCel <4.3–4.91 H9c2 < 4.3–4.77 |
<4.3–4.88 |
| B | 8 | 5 | AmMac 5.21–5.68 InfCel 4.91–5.19 Mac <4.3–4.6 |
8 | AmCel 5.16–5.73 InfCel 4.74–5.38 H9c2 < 4.3–4.52 |
<4.3–5.13 |
| C | 58 | 10 | AmMac 5.0–6.47 InfCel 4.62–6.32 Mac <4.3–4.87 |
23 | AmCel 5.02–7.98 InfCel <4.3–7.64 H9c2 < 4.3–4.96 |
<4.3–7.41 |
| D | 3 | 1 | AmMac 5.09 InfCel 5.03 Mac <4.3 |
3 | AmCel 6.18–6.65 InfCel 5.81–6.37 H9c2 < 4.3 |
5.54–6.06 |
| E | 13 | 1 | AmMac 6.28 InfCel 5.62 Mac 4.9 |
7 | AmCel 5.06–6.77 InfCel <4.3–6.68 H9c2 < 4.3–4.42 |
<4.3–6.24 |
| F | 13 | 4 | AmMac 5.0–5.85 InfCel <4.3–5.15 Mac <4.3–4.86 |
10 | AmCel 5.04–6.63 InfCel 4.43–6.24 H9c2 < 4.3–4.51 |
4.35–5.92 |
| G | 2 | 1 | AmMac 5.01 InfCel 4.31 Mac 4.74 |
2 | AmCel 6.02–6.45 InfCel 5.82–6.13 H9c2 < 4.3–4.41 |
5.41–5.84 |
| H | 19 | 1 | AmMac 5.44 InfCel 5.39 Mac 4.51 |
6 | AmCel 5.05–6.68 InfCel 4.97–6.49 H9c2 < 4.3–4.4 |
<4.3–5.59 |
| I | 5 | 0 | - - | 3 | AmCel 5.07–6.85 InfCel <4.3–6.48 H9c2 < 4.3–4.51 |
<4.3–6.33 |