Assay Detail
Binding
CHEMBL665589
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Inhibitory activity against Toxoplasma gondii Dihydrofolate reductase
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
2,4-Diamino-5-substituted-quinazolines as inhibitors of a human dihydrofolate reductase with a site-directed mutation at position 22 and of the dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.42 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.00 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 7.77 |
| CHEMBL341703 | — | — | 1 | 6.43 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 6.41 |
| CHEMBL441298 | — | — | 1 | 6.03 |
| CHEMBL164845 | — | — | 1 | 5.92 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 5.57 |
| CHEMBL349149 | — | — | 1 | 5.23 |
| CHEMBL162312 | — | — | 1 | - |
| CHEMBL434097 | — | — | 1 | - |
| CHEMBL350730 | — | — | 1 | - |
| CHEMBL162270 | — | — | 1 | - |
| CHEMBL355151 | — | — | 1 | - |
| CHEMBL165955 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL341703 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL441298 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL164845 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL349149 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL162312 | — | IC50 | > | 18000.0 | nM | - |
| CHEMBL434097 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL350730 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL162270 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL355151 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL165955 | — | IC50 | > | 20000.0 | nM | - |