Table 1.
In vitro activity of BDP inhibitors against asexual stage P. falciparum Dd2 parasites.
| Compound | Structure | cLog P | IC50PfDd2 (μM) | Compound | Structure | cLog P | IC50PfDd2 (μM) |
|---|---|---|---|---|---|---|---|
| Chloroquine |  |
4.63 | 0.11 (±0.04) | OSSL_258894b |  |
2.29 | 33.87 (±4.52) |
| Bromosporinea |  |
1.67 | 26.33 (±7.13) | OSSL_258896b |  |
3.16 | 33.98 (±21.38) |
| CPI-203a |  |
3.28 | 81.43 (±13.68) | OSSL_258897b |  |
3.37 | 35.00 (±0.00) |
| PFI-4a |  |
2.35 | 26.43 (±3.82) | OSSL_258891b |  |
2.99 | 40.78 (±28.87) |
| SGC-CBP30a |  |
5.09 | 10.03 (±0.32) | OSSL_258895b |  |
2.75 | 47.43 (±8.06) |
| OSSK_842646b |  |
4.83 | 11.28 (±2.00) | OSSL_258907b |  |
2.43 | 71.77 (±20.41) |
| OSSK_764253b |  |
3.07 | 32.45 (±15.98) | OSSL_258903b |  |
4.77 | >100 |
| OSSK_764205b |  |
3.65 | 20.23 (±1.60) | OSSL_258893b |  |
3.32 | >100 |
| OSSK_995759b |  |
2.77 | 43.24 (±12.43) | OSSL_158302b |  |
4.78 | 14.70 (±0.00) |
| OSSL_308235b |  |
1.73 | 53.83 (±17.10) | OSSK_711135b |  |
3.20 | >100 |
| OSSK_764265b |  |
1.64 | 57.30 (±19.34) | OSSK_711274b |  |
4.63 | 36.93 (±20.19) |
| OSSK_764219b |  |
1.35 | 72.40 (±3.35) | OSSK_711212b |  |
2.35 | 87.35 (±1.67) |
| OSSK_764195b |  |
2.79 | 72.88 (±8.79) | OSSK_711203b |  |
4.33 | >100 |
| OSSK_764277b |  |
1.86 | 81.25 (±12.64) | OSSL_094251b |  |
4.59 | 23.25 (±6.15) |
| OSSK_842567b |  |
4.21 | >100 | OSSK_442833b |  |
3.46 | 48.06 (±6.79) |
| OSSK_711132b |  |
2.29 | >100 | OSSL_094246b |  |
2.90 | >100 |
| OSSK_447894b |  |
1.91 | >100 | OSSK_287503b |  |
3.12 | >100 |
| OSSL_326023b |  |
2.79 | >100 | OSSK_695521b |  |
3.61 | 59.60 (±26.44) |
| OSSL_258906b |  |
3.54 | 11.80 (±3.06) | OSSL_094264b |  |
1.57 | >100 |
| OSSL_258905b |  |
5.24 | 28.82 (±4.58) | OSSK_446201b |  |
3.91 | 97.20 (±0.00) |
| OSSL_258904b |  |
2.90 | 26.03 (±2.24) | OSSK_310407b |  |
4.40 | >100 |
| OSSL_258898b |  |
3.56 | 28.17 (±4.79) |
a
Purchased from Selleck Chemicals.
b
Purchased from Princeton Biomolecular Research Inc.