Assay Detail
Binding
CHEMBL664913
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Inhibition against Dihydrofolate reductase in Toxoplasma gondii
16
Total Activities
16
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
Effect of N9-methylation and bridge atom variation on the activity of 5-substituted 2,4-diaminopyrrolo[2,3-d]pyrimidines against dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.23 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.00 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.00 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.85 |
| CHEMBL17287 | — | — | 1 | 6.82 |
| CHEMBL17232 | — | — | 1 | 6.68 |
| CHEMBL17479 | — | — | 1 | 6.09 |
| CHEMBL278261 | — | — | 1 | 6.06 |
| CHEMBL278013 | — | — | 1 | 6.00 |
| CHEMBL276734 | — | — | 1 | 5.96 |
| CHEMBL17873 | — | — | 1 | 5.85 |
| CHEMBL17323 | — | — | 1 | 5.77 |
| CHEMBL17431 | — | — | 1 | 5.58 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 5.57 |
| CHEMBL17453 | — | — | 1 | 5.47 |
| CHEMBL275893 | — | — | 1 | 5.04 |
| CHEMBL17430 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL17287 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL17232 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL17479 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL278261 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL278013 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL276734 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL17873 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL17323 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL17431 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL17453 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL275893 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL17430 | — | IC50 | = | 11600.0 | nM | 4.94 |