Assay Detail
Binding
CHEMBL665585
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant Dihydrofolate reductase from Toxoplasma gondii (tgDHFR)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Toxoplasma gondii |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL2425) ↗| Type | SINGLE PROTEIN |
| Organism | Toxoplasma gondii |
Publication
Structure-based design and synthesis of lipophilic 2,4-diamino-6-substituted quinazolines and their evaluation as inhibitors of dihydrofolate reductases and potential antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.91 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325434 | — | — | 1 | 8.41 |
| CHEMBL115804 | — | — | 1 | 8.41 |
| CHEMBL114354 | — | — | 1 | 8.39 |
| CHEMBL113816 | — | — | 1 | 8.33 |
| CHEMBL117750 | — | — | 1 | 8.27 |
| CHEMBL114839 | — | — | 1 | 7.05 |
| CHEMBL114833 | — | — | 1 | 6.27 |
| CHEMBL114058 | — | — | 1 | 6.12 |
| CHEMBL116200 | — | — | 1 | 6.11 |
| CHEMBL116637 | — | — | 1 | 6.09 |
| CHEMBL116815 | — | — | 1 | 6.08 |
| CHEMBL113999 | — | — | 1 | 6.04 |
| CHEMBL116816 | — | — | 1 | 5.96 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325434 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL115804 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL114354 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL113816 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL117750 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL114839 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL114833 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL114058 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL116200 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL116637 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL116815 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL113999 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL116816 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 6800.0 | nM | 5.17 |