Assay Detail
Binding
CHEMBL911102
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Inhibition of recombinant Plasmodium falciparum DHODH
28
Total Activities
15
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Dihydroorotate dehydrogenase (CHEMBL3486) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum |
Publication
Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.53 | 6.80 |
| Ki | 13 | 6.19 | 8.61 |
| Km | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL387254 | — | — | 2 | 8.61 |
| CHEMBL218467 | — | — | 2 | 7.70 |
| CHEMBL217951 | — | — | 2 | 7.70 |
| CHEMBL217893 | — | — | 2 | 7.52 |
| CHEMBL218703 | — | — | 2 | 7.30 |
| CHEMBL435137 | — | — | 2 | 5.50 |
| CHEMBL219856 | — | — | 2 | 5.34 |
| CHEMBL217897 | — | — | 2 | 5.00 |
| CHEMBL973 | TERIFLUNOMIDE | 4.0 | 2 | 4.63 |
| CHEMBL219855 | — | — | 2 | 4.40 |
| CHEMBL413583 | — | — | 2 | 4.40 |
| CHEMBL373493 | — | — | 2 | - |
| CHEMBL374338 | — | — | 2 | - |
| CHEMBL75782 | DIHYDROOROTATE | — | 1 | - |
| CHEMBL217894 | DECYLUBIQUINONE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL387254 | — | Ki | = | 2.45 | nM | 8.61 |
| CHEMBL218467 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL217951 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL217893 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL218703 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL218467 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL217951 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL217893 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL218703 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL435137 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL219856 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL217897 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL387254 | — | IC50 | = | 21300.0 | nM | 4.67 |
| CHEMBL973 | TERIFLUNOMIDE | Ki | = | 23350.0 | nM | 4.63 |
| CHEMBL435137 | — | IC50 | = | 27780.0 | nM | 4.56 |
| CHEMBL219855 | — | Ki | = | 40200.0 | nM | 4.40 |
| CHEMBL413583 | — | Ki | = | 39700.0 | nM | 4.40 |
| CHEMBL219856 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL217897 | — | IC50 | = | 86700.0 | nM | 4.06 |
| CHEMBL373493 | — | Ki | - | — | - | |
| CHEMBL217894 | DECYLUBIQUINONE | Km | = | 13.4 | — | - |
| CHEMBL374338 | — | Ki | - | — | - | |
| CHEMBL75782 | DIHYDROOROTATE | Km | = | 31.4 | — | - |
| CHEMBL413583 | — | IC50 | = | 345600.0 | nM | - |
| CHEMBL219855 | — | IC50 | = | 349100.0 | nM | - |
| CHEMBL374338 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL373493 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL973 | TERIFLUNOMIDE | IC50 | = | 190100.0 | nM | - |