Assay Detail
Binding
CHEMBL665451
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Inhibitory concentration against Rat liver Dihydrofolate reductase
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological activities of conformationally restricted, tricyclic nonclassical antifolates as inhibitors of dihydrofolate reductases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.32 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.82 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL50514 | — | — | 1 | 8.12 |
| CHEMBL57682 | — | — | 1 | 7.07 |
| CHEMBL299927 | — | — | 1 | 6.80 |
| CHEMBL293512 | — | — | 1 | 6.62 |
| CHEMBL58597 | — | — | 1 | 6.33 |
| CHEMBL431740 | — | — | 1 | 6.30 |
| CHEMBL60968 | — | — | 1 | - |
| CHEMBL57637 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL50514 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL57682 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL299927 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL293512 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL58597 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL431740 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL60968 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL57637 | — | IC50 | > | 2700.0 | nM | - |