Table 1. Biochemical and larvicidal properties of the most potent PTFs.
| PTFa | Groupa | IC50 (µM)b | Mortality at 300 µMc | ||||
| WT | G119S | RIC50 b | Slab | SR | Rm300 c | ||
| 33f | B | 490.0 | 22.0 | 22.3 | 16% | 77% | 4.8 |
| 52 | C | 860.0 | 52.0 | 16.5 | 0% | 0% | − |
| 8f | A | 312.0 | 19.0 | 16.4 | 60% | 100% | 1.7 |
| 25 d,f | B | 442.0 | 28.6 | 15.5 | 32% | 68% | 2.1 |
| 37 | B | 2121.0 | 142.0 | 14.9 | 0% | 35% | − |
| 7 | A | 424.0 | 35.0 | 12.1 | 100% | 100% | 1.0 |
| 20 d,f | A | 330.0 | 27.5 | 12.0 | 43% | 94% | 2.2 |
| 39 d,f | C | 74.3 | 7.6 | 9.8 | 29% | 81% | 2.8 |
| 69 | F | 43.9 | 4.6 | 9.5 | 0% | 0% | − |
| 12 | A | 54.0 | 6.0 | 9.0 | 46% | 88% | 1.9 |
| 4 | A | 111.0 | 14.0 | 7.9 | 78% | 100% | 1.3 |
| 10 d,f | A | 592.0 | 81.4 | 7.3 | 14% | 87% | 6.2 |
| 16 | A | 260.0 | 37.0 | 7.0 | 80% | 100% | 1.3 |
| 60 | D | 7.7 | 1.1 | 6.8 | 50% | 50% | 1.0 |
| 9f | A | 132.0 | 21.5 | 6.1 | 19% | 39% | 2.1 |
| 3 d,f | A,D | 29.4 | 6.2 | 4.7 | 43% | 78% | 1.8 |
| 29 d,f | B | 118.0 | 33.5 | 3.5 | 27% | 63% | 2.3 |
| 38 | C | 1189.0 | 357.0 | 3.3 | 70% | 90% | 1.3 |
| 45 | C | 3.4 | 1.1 | 3.1 | 0% | 0% | − |
| 18 | A | 5.3 | 1.8 | 2.9 | 0% | 0% | − |
| 70 | F | 18.0 | 6.2 | 2.9 | 0% | 0% | − |
| 13f | A | 236.0 | 89.0 | 2.7 | 64% | 96% | 1.5 |
| 56 | D | 4.9 | 1.9 | 2.6 | 0% | 0% | − |
| 59 | D | 45.7 | 18.5 | 2.5 | 0% | 0% | − |
| 47 | C | 3.0 | 1.3 | 2.3 | 0% | 0% | − |
| 2f | A | 12.6 | 5.5 | 2.3 | 12% | 53% | 4.4 |
| 30 | B | 2.8 | 1.3 | 2.2 | 25% | 25% | 1.0 |
| 57 | D | 11.3 | 5.4 | 2.1 | 0% | 0% | − |
| 66f | F | 91.6 | 51.0 | 1.8 | 63% | 100% | 1.6 |
| 35 | B | 8.7 | 8.7 | 1.0 | 5% | 49% | 9.8 |
| 23 | B | 12.1 | 15.5 | 0.8 | 24% | 60% | 2.5 |
| 24e | B | 1.3 | 1.9 | 0.7 | 0% | 0% | − |
| 17 | A | 5.0 | 8.0 | 0.6 | 15% | 90% | 6.0 |
a
numbers and groups refer to Table S1.
b
IC50 values were determined from regression analysis of log-concentrations versus percentage inhibitions. RIC50 = IC50 WT/IC50 G119S. Compounds were sorted by their RIC50 ratio.
c
Mortality was measured from bioassays on Slab (OP-sensitive) and SR (OP-insensitive) strains exposed for 24 hours to 300 µM PTF. Rm300 = SR mortality/Slab mortality.
d
PTFs biochemically characterized are in bold.
e
Hit compound from the primary screen.
f
Compounds with RIC50 and Rm300 above 1.5.