Assay Detail
Binding
CHEMBL667607
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against Dihydrofolate reductase enzyme purified from Plasmodium berghei.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium berghei |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL3963) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium berghei str. ANKA |
Publication
2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 2. C-Alkylation of pyrimidines with Mannich bases and application to the synthesis of trimethoprim and analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.56 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 6.92 |
| CHEMBL1181 | 4-HYDROXYTRIMETHOPRIM | — | 1 | 6.52 |
| CHEMBL325533 | — | — | 1 | 6.47 |
| CHEMBL339058 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1181 | 4-HYDROXYTRIMETHOPRIM | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL325533 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL339058 | — | IC50 | = | 480.0 | nM | 6.32 |