Table 1 C. elegans chemical screening results—summary of NPD bioactivity
From: Identification of a family of species-selective complex I inhibitors as potential anthelmintics
Bioactivity | ||||||
|---|---|---|---|---|---|---|
Compound ID | Library | Hit Type | Structural Group | C. elegans KCN Survival Assay LC50 (μM) | C. elegans Dev. & Viability Assay LC50 (μM) | HEK293 Cell Viability Assay LC50 (μM) |
Rotenone | Control | NA | – | 0.86 | 3.39 | <0.39 |
Wact-11 | Control | NA | – | 4.43 | 0.42 | >50 |
Siccanin | Authentic | KCN | – | 6.34 | 15.23 | 22.21 |
Niclosamide | Authentic | KCN | – | 0.095 | >1000 | – |
Flunarizine | Authentic | KCN | – | 21.98 | >200 | 30.23 |
Nocodazole | Authentic | Dev. & Viability | – | – | – | – |
Staurosporine | Authentic | Dev. & Viability | – | – | – | – |
Camptothecin | Authentic | Dev. & Viability | – | – | – | – |
Reveromycin A | Authentic | Dev. & Viability | – | – | – | – |
Aristolochic acid | Authentic | Dev. & Viability | – | – | – | – |
NPD6621 | Pilot | KCN | 1 | 48.03 | – | – |
NPD8902 | Deriv./Analog | KCN | 1 | 28.26 | >100 | 23.54 |
NPD6380 | Pilot | KCN | 2 | 14.35 | >100 | 29.20 |
NPD8034 | Deriv./Analog | KCN | 2 | 11.97 | >100 | 11.15 |
NPD6383 | Deriv./Analog | KCN | 2 | 22.24 | – | – |
NPD601 | Deriv./Analog | KCN | 2 | 13.60 | – | – |
NPD1450 | Deriv./Analog | KCN | 2 | 35.28 | >100 | >50 |
NPD8366 | Pilot | KCN | 3 | 11.62 | >100 | 19.73 |
NPD8582 | Deriv./Analog | KCN | 3 | 14.70 | – | – |
NPD6240 | Deriv./Analog | KCN | 3 | 7.60 | >100 | 24.76 |
FSL0005 | Deriv./Analog | KCN | 3 | 0.93 | 4.18 | 7.48 |
NPD8298 | Deriv./Analog | KCN | 3 | 2.57 | >100 | >50 |
NPD10504 | Pilot | KCN | 4 | 15.59 | >100 | 36.63 |
NPD3577 | Deriv./Analog | KCN | 4 | 15.95 | >100 | 21.43 |
NPD6303 | Deriv./Analog | KCN | 4 | 32.20 | >100 | 33.35 |
NPD8790 | Deriv./Analog | KCN | 4 | 14.27 | >100 | >50 |
Anacardic acid | Pilot | KCN | 5 | 3.35 | >100 | >50 |
6-heptadeca-9Z,12Z-dienyl salicylic acid | Deriv./Analog | KCN | 5 | 3.97 | – | – |
NPD10211 | Pilot | KCN/Dev. & Viability | 6 | 14.46 | – | – |
NPD390 | Deriv./Analog | KCN/Dev. & Viability | 6 | 16.56 | 45.27 | 3.20 |
NP974 | Deriv./Analog | KCN/Dev. & Viability | 6 | 18.96 | – | – |
NPL50654-01 | Pilot | KCN/Dev. & Viability | 7 | 7.81 | 29.38 | 3.20 |
NPD5176 | Pilot | Dev. & Viability | 8 | – | 83.32 | >50 |
NPD5219 | Pilot | Dev. & Viability | 9 | – | 38.73 | 14.84 |
HTD0465 | Pilot | Dev. & Viability | 10 | – | 35.32 | 20.46 |
STK418118 | Pilot | Dev. & Viability | 11 | – | 43.27 | >50 |
