Assay Detail
Binding
CHEMBL669249
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Inhibitory activity against dihydrofolate reductase (DHFR) enzyme from Escherichia coli
9
Total Activities
9
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 as antibacterial agents. 8. The 3,4,5-triethyl isostere of trimethoprim. A study of specificity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.89 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 8.30 |
| CHEMBL57582 | — | — | 1 | 8.00 |
| CHEMBL19633 | DIAVERIDINE | 2.0 | 1 | 7.30 |
| CHEMBL293013 | — | — | 1 | 7.05 |
| CHEMBL60883 | — | — | 1 | 6.55 |
| CHEMBL59703 | — | — | 1 | 6.40 |
| CHEMBL19023 | — | — | 1 | 6.30 |
| CHEMBL60029 | — | — | 1 | 6.19 |
| CHEMBL61287 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL57582 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL19633 | DIAVERIDINE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL293013 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL60883 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL59703 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL19023 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL60029 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL61287 | — | IC50 | = | 1100.0 | nM | 5.96 |