Assay Detail
Functional
CHEMBL3430851
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MMV: Gametocytes from P. falciparum reporter strain NF54-deltaPf47-5'hsp70-GFP::Luc were exposed to serial dilutions of compounds for 24 hours. Subsequently, compounds were washed out and gametocytes were fed to Anopheles stephensi mosquitoes. Three compounds were tested at six dilutions in one experimental run. All conditions were tested in duplicate in two different experimental runs. Each run included duplicate feeders for vehicle (0.1% DMSO) and positive (10 uM dihydroartemisinin) controls. Eight days post-feeding, oocyst densities were determined by assessment of luminescence signals in homogenized mosquitoes. Up to 24 mosquitoes were analysed per feeder. Luminescence data from individual mosquitoes were normalized against the average signals from the vehicle control feeds that were included in each run. IC50 values were determined by fitting a four-parameter logistic regression model using maximum likelihood optimization to find the best fit.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
MMV Malaria Box gametocyte standard membrane feeding assay screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.19 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL592105 | METHYLROSANILINE | -1.0 | 1 | 7.41 |
| CHEMBL1437888 | — | — | 1 | 7.23 |
| CHEMBL582767 | — | — | 1 | 7.13 |
| CHEMBL586310 | — | — | 1 | 7.02 |
| CHEMBL206540 | — | — | 1 | 6.96 |
| CHEMBL592550 | — | — | 1 | 6.23 |
| CHEMBL546799 | — | — | 1 | 5.93 |
| CHEMBL124006 | — | — | 1 | 5.93 |
| CHEMBL261693 | — | — | 1 | 5.90 |
| CHEMBL532597 | — | — | 1 | 5.89 |
| CHEMBL601156 | — | — | 1 | 5.85 |
| CHEMBL537087 | — | — | 1 | 5.78 |
| CHEMBL601325 | — | — | 1 | 5.76 |
| CHEMBL526800 | — | — | 1 | 5.49 |
| CHEMBL1460047 | — | — | 1 | 5.44 |
| CHEMBL530308 | — | — | 1 | 5.07 |
| CHEMBL533017 | — | — | 1 | - |
| CHEMBL588481 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL592105 | METHYLROSANILINE | IC50 | = | 38.9 | nM | 7.41 |
| CHEMBL1437888 | — | IC50 | = | 58.88 | nM | 7.23 |
| CHEMBL582767 | — | IC50 | = | 74.13 | nM | 7.13 |
| CHEMBL586310 | — | IC50 | = | 95.5 | nM | 7.02 |
| CHEMBL206540 | — | IC50 | = | 109.65 | nM | 6.96 |
| CHEMBL592550 | — | IC50 | = | 588.84 | nM | 6.23 |
| CHEMBL546799 | — | IC50 | = | 1174.9 | nM | 5.93 |
| CHEMBL124006 | — | IC50 | = | 1174.9 | nM | 5.93 |
| CHEMBL261693 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL532597 | — | IC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL601156 | — | IC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL537087 | — | IC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL601325 | — | IC50 | = | 1737.8 | nM | 5.76 |
| CHEMBL526800 | — | IC50 | = | 3235.94 | nM | 5.49 |
| CHEMBL1460047 | — | IC50 | = | 3630.78 | nM | 5.44 |
| CHEMBL530308 | — | IC50 | = | 8511.38 | nM | 5.07 |
| CHEMBL533017 | — | IC50 | - | — | - | |
| CHEMBL588481 | — | IC50 | - | — | - |