Assay Detail
Binding
CHEMBL665444
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Inhibitory activity against rat dihydrofolate reductase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.12 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.48 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.10 |
| CHEMBL37334 | — | — | 1 | 5.66 |
| CHEMBL300419 | — | — | 1 | 5.30 |
| CHEMBL34293 | — | — | 1 | 5.09 |
| CHEMBL52415 | — | — | 1 | 4.06 |
| CHEMBL53193 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL37334 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL300419 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL34293 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL52415 | — | IC50 | = | 88000.0 | nM | 4.06 |
| CHEMBL53193 | — | IC50 | = | 180000.0 | nM | - |