TABLE 1.
Collated PfIVT and counterscreen data for compounds from MMV’s Pathogen Box demonstrating >50% inhibition in a single-point IVT screen at 30 μMa
| Compound | PfIVT inhibition at 30 μM (%) | IC50 value (μM) |
||
|---|---|---|---|---|
| PfIVT | HsIVT | Counterscreen | ||
| MMV688407 | 98.7 | 6 ± 0.09 | 5.2 ± 0.02 | >30 |
| MMV667494 | 97.7 | 0.3 ± 0.09 | >30 | >30 |
| MMV688991 | 97.0 | 0.02 ± 0.008 | 0.04 ± 0.0003 | 0.02 ± 0.008 |
| MMV688547 | 96.7 | 1.8 ± 0.07 | 2.7 ± 0.02 | >30 |
| MMV687807 | 95.1 | 0.09 ± 0.007 | 0.5 ± 0.006 | 25 ± 0.8 |
| MMV688362 | 93.5 | 2.8 ± 0.08 | 5.6 ± 0.04 | >30 |
| MMV634140 | 88.4 | 2.9 ± 0.09 | >30 | >30 |
| MMV019189 | 84.4 | 0.03 ± 0.009 | 7.7 ± 0.3 | 7 ± 0.6, (>30) |
| MMV687243 | 82.5 | 2.2 ± 0.08 | 13 ± 0.2 | 0.9 ± 0.09 |
| MMV637953 | 78.7 | 3.1 ± 0.07 | >30 | >30 |
| MMV688474 | 78.4 | 16 ± 0.9 | 14 ± 0.07 | >30 |
| MMV676008 | 74.9 | 0.4 ± 0.08 | 12 ± 0.4 | 21 ± 0.6 |
| MMV687730 | 72.4 | 3.9 ± 0.8 | >30 | >30 |
| MMV675998 | 68.9 | 13 ± 0.9 | 18 ± 0.13 | >30 |
| MMV688271 | 65.7 | 18 ± 0.9 | 13 ± 0.16 | >30 |
| MMV676350 | 65.1 | 16 ± 0.8 | 6.7 ± 0.13 | >30 |
| MMV687188 | 64.9 | 2.4 ± 0.07 (>30) | >30 | >30 |
| MMV688372 | 62.9 | 0.6 ± 0.06 | >30 | 11 ± 0.8 (>30) |
| MMV676512 | 54.2 | >30 | 22 ± 0.46 | >30 |
a
All IC50 values represent the weighted means ± standard deviations of two technical replicates. Compounds with IC50 values 1 order of magnitude (10-fold) higher for the counterscreen than for the PfIVT assay are considered viable hits and are shaded.