Assay Detail
Functional
CHEMBL2174378
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Antiplasmodial activity against Plasmodium falciparum Dd2 assessed as inhibition of [3H]hypoxanthine incorporation incubated for 24 hrs prior to [3H]hypoxanthine addition measured after 24 hrs by beta scintillation counting
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.65 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2169991 | — | — | 1 | 8.00 |
| CHEMBL269671 | ARTEMISININ | 3.0 | 1 | 7.70 |
| CHEMBL2169990 | — | — | 1 | 7.70 |
| CHEMBL2172623 | — | — | 1 | 7.40 |
| CHEMBL2172621 | — | — | 1 | 6.85 |
| CHEMBL2169981 | — | — | 1 | 6.68 |
| CHEMBL2172619 | — | — | 1 | 6.19 |
| CHEMBL76 | CHLOROQUINE | 4.0 | 1 | 6.15 |
| CHEMBL2169988 | — | — | 1 | 6.10 |
| CHEMBL2169982 | — | — | 1 | 6.09 |
| CHEMBL2169977 | — | — | 1 | 5.97 |
| CHEMBL14368 | — | — | 1 | 5.96 |
| CHEMBL14276 | — | — | 1 | 5.67 |
| CHEMBL2169980 | — | — | 1 | - |
| CHEMBL2169979 | — | — | 1 | - |
| CHEMBL2169978 | — | — | 1 | - |
| CHEMBL2169976 | — | — | 1 | - |
| CHEMBL2172622 | — | — | 1 | - |
| CHEMBL2172620 | — | — | 1 | - |
| CHEMBL2169992 | — | — | 1 | - |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | - |
| CHEMBL2169989 | — | — | 1 | - |
| CHEMBL2169987 | — | — | 1 | - |
| CHEMBL586213 | — | — | 1 | - |
| CHEMBL2169986 | — | — | 1 | - |
| CHEMBL2169985 | — | — | 1 | - |
| CHEMBL14255 | — | — | 1 | - |
| CHEMBL2169984 | — | — | 1 | - |
| CHEMBL2169983 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2169991 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL269671 | ARTEMISININ | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2169990 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2172623 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2172621 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2169981 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2172619 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL76 | CHLOROQUINE | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL2169988 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2169982 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL2169977 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL14368 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL14276 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL2169980 | — | IC50 | - | — | - | |
| CHEMBL2169979 | — | IC50 | - | — | - | |
| CHEMBL2169978 | — | IC50 | - | — | - | |
| CHEMBL2169976 | — | IC50 | - | — | - | |
| CHEMBL2172622 | — | IC50 | - | — | - | |
| CHEMBL2172620 | — | IC50 | - | — | - | |
| CHEMBL2169992 | — | IC50 | - | — | - | |
| CHEMBL36 | PYRIMETHAMINE | IC50 | > | 40000.0 | nM | - |
| CHEMBL2169989 | — | IC50 | - | — | - | |
| CHEMBL2169987 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL586213 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2169986 | — | IC50 | - | — | - | |
| CHEMBL2169985 | — | IC50 | - | — | - | |
| CHEMBL14255 | — | IC50 | - | — | - | |
| CHEMBL2169984 | — | IC50 | - | — | - | |
| CHEMBL2169983 | — | IC50 | - | — | - |