Assay Detail
Binding
CHEMBL666803
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Inhibitory activity against dihydrofolate reductase in humans
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
The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.95 | 9.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 9.75 |
| CHEMBL284943 | — | — | 1 | 8.84 |
| CHEMBL35427 | — | — | 1 | 8.79 |
| CHEMBL35364 | — | — | 1 | 8.71 |
| CHEMBL285474 | — | — | 1 | 6.88 |
| CHEMBL35552 | — | — | 1 | 6.34 |
| CHEMBL265757 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | Ki | = | 0.179 | nM | 9.75 |
| CHEMBL284943 | — | Ki | = | 1.45 | nM | 8.84 |
| CHEMBL35427 | — | Ki | = | 1.63 | nM | 8.79 |
| CHEMBL35364 | — | Ki | = | 1.97 | nM | 8.71 |
| CHEMBL285474 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL35552 | — | Ki | = | 453.0 | nM | 6.34 |
| CHEMBL265757 | — | Ki | = | 485.0 | nM | 6.31 |