Assay Detail
Binding
CHEMBL665587
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against DHFR (Dihydrofolate reductase) from Toxoplasma gondii.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Toxoplasma gondii |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL2425) ↗| Type | SINGLE PROTEIN |
| Organism | Toxoplasma gondii |
Publication
Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.92 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.00 |
| CHEMBL423200 | — | — | 1 | 7.92 |
| CHEMBL144839 | — | — | 1 | 7.54 |
| CHEMBL301769 | — | — | 1 | 7.37 |
| CHEMBL144200 | — | — | 1 | 6.96 |
| CHEMBL342086 | — | — | 1 | 6.04 |
| CHEMBL424113 | — | — | 1 | 5.89 |
| CHEMBL423381 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL423200 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL144839 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL301769 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL144200 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL342086 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL424113 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL423381 | — | IC50 | = | 2200.0 | nM | 5.66 |