ID | % inhibition, PfNF54-Luc at 3 µM | IC50 [µM], Pf3D7 + solvent | IC50 [µM], Pf3D7 + 0.8 mM CoA | IC50-ratio (CoA/solvent) | IC50 [µM], THP-1 | IC50 [µM], HEK-293 |
---|---|---|---|---|---|---|
3a | 80.8 ± 0.5 | 0.283 ± 0.073 | 4.61 ± 0.15 | 16.3 | 6.13 | >10 |
3b | 25.7 ± 2.0 at 30 µM | nd | nd | – | nd | nd |
3c | 37.3 ± 3.7 at 30 µM | nd | nd | – | nd | nd |
3d | −0.6 ± 5.4 | nd | nd | – | nd | nd |
3e | −7.3 ± 6.9 | nd | nd | – | nd | nd |
3f | 1.5 ± 4.3 | nd | nd | – | nd | nd |
3g | −13.1 ± 9.1 | nd | nd | – | nd | nd |
3h | −103.3 ± 4.4 | nd | nd | – | nd | nd |
3i | −5.5 ± 3.8 | nd | nd | – | nd | nd |
3j | −11.0 ± 6.7 | nd | nd | – | nd | nd |
3k | −7.0 ± 1.8 | nd | nd | – | nd | nd |
3l | 24.3 ± 3.2 | nd | nd | – | nd | nd |
3m | −8.3 ± 4.1 | nd | nd | – | nd | nd |
3n | −0.82 ± 3.11 | nd | nd | – | nd | nd |
3o | 2.28 ± 3.31 | nd | nd | – | nd | nd |
3p | −14.6 ± 12.9 | nd | nd | – | nd | nd |
3q | −12.3 ± 2.2 | nd | nd | – | nd | nd |
3r | 7.7 ± 1.8 | nd | nd | – | nd | nd |
3s | −2.8 ± 16.6 | nd | nd | – | nd | nd |
6a | −24.8 ± 13.6 | nd | nd | – | nd | nd |
6b | 1.79 ± 2.53 | nd | nd | – | nd | nd |
6c | 0.98 ± 1.52 | nd | nd | – | nd | nd |
8a | 33.2 ± 6.8 | 10.5 ± 1.1 | 16.1 ± 2.2 | 1.53 | nd | >40 |
8b | 4.7 ± 2.6 | 5.37 ± 1.0 | 39.7 ± 0.7 | 7.39 | nd | >40 |
8c | 96.5 ± 1.6 | 1.26 ± 0.16 | 2.31 ± 0.17 | 1.83 | >300 | >40 |
8d | 99.9 ± 0.0 | 0.0388 ± 0.0010 | 2.61 ± 0.42 | 67.3 | 27.5 | >10 |
8e | 99.5 ± 0.5 | 0.0747 ± 0.021 | 2.58 ± 0.42 | 34.5 | 33.6 | >10 |
8f | 99.7 ± 0.1 | 0.0958 ± 0.0063 | 11.2 ± 2.6 | 117 | 11 | >4 |
8g | 95.0 ± 1.1 | 0.0734 ± 0.0022 | 0.531 ± 0.007 | 7.23 | 16.5 | >10 |
8h | −1.9 ± 5.3 | nd | nd | – | nd | nd |
8i | −18.4 ± 10.6 | nd | nd | – | nd | nd |
8j | −36.3 ± 10.6 | nd | nd | – | nd | nd |
8k | 98.0 ± 0.2 | 0.149 ± 0.021 | 1.06 ± 0.03 | 7.11 | 28 | >20 |
BS | 99.3 ± 0.7 | nd | nd | – | nd | nd |
Amb 180,780 | nd | 0.0370 ± 0.0017 | 1.51 ± 0.19 | 40.8 | nd | >40 |
Chloroqu | nd | 0.0195 ± 0.0034 | 0.0271 ± 0.0094 | 1.39 | nd | >40 |
Artemis | nd | 0.00337 ± 0.00065 | 0.00490 ± 0.0011 | 1.45 | nd | nd |
Puromyc | nd | 0.0338 ± 0.012 | 0.0939 ± 0.0016 | 2.78 | nd | 0.36 |
Pantoth | nd | 752 ± 82 | >10,000 | >13.3 | nd | nd |