Assay Detail
Binding
CHEMBL1073069
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Inhibition of Toxoplasma gondii DHFR at 37 degC by spectrophotometry
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 | Autocuration |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL2425) ↗| Type | SINGLE PROTEIN |
| Organism | Toxoplasma gondii |
Publication
2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 4.85 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.00 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 5.55 |
| CHEMBL596672 | — | — | 1 | 4.92 |
| CHEMBL611984 | — | — | 1 | 4.79 |
| CHEMBL609896 | — | — | 1 | 4.71 |
| CHEMBL596680 | — | — | 1 | 4.59 |
| CHEMBL596681 | — | — | 1 | 4.42 |
| CHEMBL598090 | — | — | 1 | 4.36 |
| CHEMBL598292 | — | — | 1 | 4.34 |
| CHEMBL598293 | — | — | 1 | 4.29 |
| CHEMBL597885 | — | — | 1 | 4.16 |
| CHEMBL604722 | — | — | 1 | 4.09 |
| CHEMBL596673 | — | — | 1 | - |
| CHEMBL602104 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL596672 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL611984 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL609896 | — | IC50 | = | 19700.0 | nM | 4.71 |
| CHEMBL596680 | — | IC50 | = | 25500.0 | nM | 4.59 |
| CHEMBL596681 | — | IC50 | = | 38400.0 | nM | 4.42 |
| CHEMBL598090 | — | IC50 | = | 44200.0 | nM | 4.36 |
| CHEMBL598292 | — | IC50 | = | 45900.0 | nM | 4.34 |
| CHEMBL598293 | — | IC50 | = | 51700.0 | nM | 4.29 |
| CHEMBL597885 | — | IC50 | = | 69400.0 | nM | 4.16 |
| CHEMBL604722 | — | IC50 | = | 81800.0 | nM | 4.09 |
| CHEMBL596673 | — | IC50 | > | 12000.0 | nM | - |
| CHEMBL602104 | — | IC50 | > | 83000.0 | nM | - |