Assay Detail
Binding
CHEMBL664375
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Inhibition of Pneumocystis carinii Dihydrofolate Reductase
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Pneumocystis carinii |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
2,4-Diaminothieno[2,3-d]pyrimidine lipophilic antifolates as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.68 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31891 | BRODIMOPRIM | 2.0 | 1 | 7.51 |
| CHEMBL280378 | EPIROPRIM | 2.0 | 1 | 7.38 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 5.43 |
| CHEMBL331351 | — | — | 1 | 5.12 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 4.92 |
| CHEMBL331682 | — | — | 1 | 4.89 |
| CHEMBL122214 | — | — | 1 | 4.51 |
| CHEMBL122259 | — | — | 1 | - |
| CHEMBL433021 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31891 | BRODIMOPRIM | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL280378 | EPIROPRIM | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL331351 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL331682 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL122214 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL122259 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL433021 | — | IC50 | > | 10000.0 | nM | - |