Assay Detail
Binding
CHEMBL668123
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Inhibitory activity against Dihydrofolate reductase enzyme purified from Escherichia coli
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Escherichia coli |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
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 | 5 | 7.06 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 8.30 |
| CHEMBL1181 | 4-HYDROXYTRIMETHOPRIM | — | 1 | 7.96 |
| CHEMBL325533 | — | — | 1 | 7.00 |
| CHEMBL339058 | — | — | 1 | 6.52 |
| CHEMBL340759 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1181 | 4-HYDROXYTRIMETHOPRIM | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL325533 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL339058 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL340759 | — | IC50 | = | 3200.0 | nM | 5.50 |