Table 1:
Compound | CID | Structure | TGR IC50 (μM) | Adult worms | Sm║ juvenile | Sm║ Somula | |||
---|---|---|---|---|---|---|---|---|---|
qHTS† | Confirm | Sm║ | Sj║ | Sh║ | |||||
1 | 3561200 | n. d.* | 0.33 | 10 μM 120 h 62% d‡ |
10 μM 120 h 65% d‡ |
10 μM 144 h 67% d‡ |
10 μM 120 h 39% d‡ |
10 μM 24 h 99% d‡ |
|
2 | 16012863 | 0.3981 | 0.21 | 10 μM 120 h 78% d‡ |
10 μM 120 h 50% d‡ |
10 μM 120 h 94% d‡ |
10 μM 24 h 100% d‡ |
10 μM 24 h 100% d‡ |
|
3 | 4412151 | 6.3^ | 2.84 | 10 μM 72 h 100% d‡ |
10 μM 120 h 70% d‡ |
10 μM 96 h 100% d‡ |
10 μM 48 h 100% d‡ |
10 μM 24 h 100% d‡ |
|
4€ | 2779853 | 5.438^ | 2.01 | 10 μM 144 h 76% d‡ |
10 μM 120 h 69% d‡ |
10 μM 120 h 85% d‡ |
10 μM 72 h 100% d‡ |
10 μM 24 h 100% d‡ |
|
5& | 2801235 | 0.1 | 0.06 | 10 μM 120 h 67% d‡ |
10 μM 120 h 30% d‡ |
10 μM 120 h 48% d‡ |
10 μM 120 h 57% d‡ |
10 μM 24 h 100% d‡ |
|
6 | 659226 | 0.631 | 0.14 | 12.5 μM 120 h 28% d‡ |
12.5 μM 120 h 100% d‡ |
n. d.* | 12.5 μM 120 h 100% d‡ |
12.5 μM 120 h 96% d‡ |
|
7 | 1090309 | 0.3162 | 0.09 | 12.5 μM 120 h 43% d‡ |
12.5 μM 120 h no killing |
n. d.* | 12.5 μM 120 h 8% d‡ |
12.5 μM 120 h 61% d‡ |
|
8 | 2943813 | 0.3981 | 0.13 | 12.5 μM 120 h 53% d‡ |
12.5 μM 120 h 56% d‡ |
n. d.* | 10 μM 120 h 24% d‡ |
10 μM 120 h 20% d‡ |