Assay Detail
Binding
CHEMBL4181680
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Inhibition of Plasmodium falciparum DHFR using DHF as substrate preincubated for 15 mins followed DHF addition measured after 15 mins by spectrophotometric method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL1939) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum K1 |
Publication
Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.18 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1939368 | — | — | 1 | 8.20 |
| CHEMBL4213489 | — | — | 1 | 7.67 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 7.59 |
| CHEMBL4207961 | — | — | 1 | 7.58 |
| CHEMBL4209975 | — | — | 1 | 7.49 |
| CHEMBL4218177 | — | — | 1 | 7.40 |
| CHEMBL4207059 | — | — | 1 | 7.30 |
| CHEMBL4213904 | — | — | 1 | 7.25 |
| CHEMBL4210479 | — | — | 1 | 7.21 |
| CHEMBL4213293 | — | — | 1 | 7.17 |
| CHEMBL4203015 | — | — | 1 | 7.15 |
| CHEMBL4210735 | — | — | 1 | 7.09 |
| CHEMBL4209486 | — | — | 1 | 7.08 |
| CHEMBL4216274 | — | — | 1 | 6.97 |
| CHEMBL4218788 | — | — | 1 | 6.93 |
| CHEMBL4214368 | — | — | 1 | 6.80 |
| CHEMBL4206536 | — | — | 1 | 6.74 |
| CHEMBL4211317 | — | — | 1 | 6.73 |
| CHEMBL4212687 | — | — | 1 | 6.65 |
| CHEMBL4211543 | — | — | 1 | 6.54 |
| CHEMBL4203128 | — | — | 1 | - |
| CHEMBL4209200 | — | — | 1 | - |
| CHEMBL4202708 | — | — | 1 | - |
| CHEMBL1458713 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1939368 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4213489 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL4207961 | — | IC50 | = | 26.2 | nM | 7.58 |
| CHEMBL4209975 | — | IC50 | = | 32.1 | nM | 7.49 |
| CHEMBL4218177 | — | IC50 | = | 39.6 | nM | 7.40 |
| CHEMBL4207059 | — | IC50 | = | 50.6 | nM | 7.30 |
| CHEMBL4213904 | — | IC50 | = | 55.6 | nM | 7.25 |
| CHEMBL4210479 | — | IC50 | = | 61.1 | nM | 7.21 |
| CHEMBL4213293 | — | IC50 | = | 67.9 | nM | 7.17 |
| CHEMBL4203015 | — | IC50 | = | 70.1 | nM | 7.15 |
| CHEMBL4210735 | — | IC50 | = | 80.9 | nM | 7.09 |
| CHEMBL4209486 | — | IC50 | = | 84.1 | nM | 7.08 |
| CHEMBL4216274 | — | IC50 | = | 107.4 | nM | 6.97 |
| CHEMBL4218788 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL4214368 | — | IC50 | = | 157.2 | nM | 6.80 |
| CHEMBL4206536 | — | IC50 | = | 180.2 | nM | 6.74 |
| CHEMBL4211317 | — | IC50 | = | 185.4 | nM | 6.73 |
| CHEMBL4212687 | — | IC50 | = | 225.5 | nM | 6.65 |
| CHEMBL4211543 | — | IC50 | = | 289.9 | nM | 6.54 |
| CHEMBL4203128 | — | IC50 | - | — | - | |
| CHEMBL4209200 | — | IC50 | - | — | - | |
| CHEMBL4202708 | — | IC50 | - | — | - | |
| CHEMBL1458713 | — | IC50 | - | — | - |