Assay Detail
Functional
CHEMBL1785544
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Antimalarial activity against Plasmodium falciparum 3D7 infected in human A positive erythrocytes by [3H]hypoxanthine uptake assay in presence of serum in medium
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 62 | 5.87 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1450 | ATOVAQUONE | 4.0 | 1 | 8.82 |
| CHEMBL76 | CHLOROQUINE | 4.0 | 1 | 8.15 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 7.64 |
| CHEMBL1784580 | — | — | 1 | 7.18 |
| CHEMBL1784574 | — | — | 1 | 7.01 |
| CHEMBL1784578 | — | — | 1 | 6.80 |
| CHEMBL1784566 | — | — | 1 | 6.57 |
| CHEMBL1784561 | — | — | 1 | 6.50 |
| CHEMBL1784563 | — | — | 1 | 6.47 |
| CHEMBL1784589 | — | — | 1 | 6.40 |
| CHEMBL600255 | — | — | 1 | 6.11 |
| CHEMBL586157 | — | — | 1 | 6.10 |
| CHEMBL1784577 | — | — | 1 | 5.96 |
| CHEMBL1784590 | — | — | 1 | 5.89 |
| CHEMBL1784567 | — | — | 1 | 5.89 |
| CHEMBL1784562 | — | — | 1 | 5.85 |
| CHEMBL1784593 | — | — | 1 | 5.75 |
| CHEMBL1784576 | — | — | 1 | 5.64 |
| CHEMBL1784711 | — | — | 1 | 5.64 |
| CHEMBL1784594 | — | — | 1 | 5.60 |
| CHEMBL582694 | — | — | 1 | 5.57 |
| CHEMBL1714424 | — | — | 1 | 5.48 |
| CHEMBL1784713 | — | — | 1 | 5.47 |
| CHEMBL1784575 | — | — | 1 | 5.46 |
| CHEMBL1784573 | — | — | 1 | 5.43 |
| CHEMBL1784556 | — | — | 1 | 5.32 |
| CHEMBL1784564 | — | — | 1 | 5.29 |
| CHEMBL1784591 | — | — | 1 | 5.18 |
| CHEMBL1784555 | — | — | 1 | 5.17 |
| CHEMBL1784592 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1450 | ATOVAQUONE | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL76 | CHLOROQUINE | EC50 | = | 7.1 | nM | 8.15 |
| CHEMBL36 | PYRIMETHAMINE | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1784580 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1784574 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL1784578 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1784566 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1784561 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1784563 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1784589 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL600255 | — | EC50 | = | 780.0 | nM | 6.11 |
| CHEMBL586157 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1784577 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1784567 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1784590 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1784562 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1784593 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1784576 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1784711 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1784594 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL582694 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1714424 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1784713 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1784575 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1784573 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL1784556 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL1784564 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL1784591 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL1784555 | — | EC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL1784592 | — | EC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL1784717 | — | EC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL1784595 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1784565 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1784710 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1784579 | — | EC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL1784581 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1784709 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1784585 | — | EC50 | - | — | - | |
| CHEMBL1784586 | — | EC50 | - | — | - | |
| CHEMBL1784587 | — | EC50 | - | — | - | |
| CHEMBL1784588 | — | EC50 | - | — | - | |
| CHEMBL1784596 | — | EC50 | - | — | - | |
| CHEMBL1784707 | — | EC50 | - | — | - | |
| CHEMBL1784570 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1784572 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1784712 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1784571 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL1784716 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1784714 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1784715 | — | EC50 | > | 10000.0 | nM | - |