Assay Detail
Binding
CHEMBL665857
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Inhibitory activity against dihydrofolate reductase from pneumocystis carinii
18
Total Activities
18
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
Selective Pneumocystis carinii dihydrofolate reductase inhibitors: design, synthesis, and biological evaluation of new 2,4-diamino-5-substituted-furo[2,3-d]pyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.12 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 7.38 |
| CHEMBL283311 | — | — | 1 | 6.19 |
| CHEMBL280378 | EPIROPRIM | 2.0 | 1 | 5.58 |
| CHEMBL23960 | — | — | 1 | 5.11 |
| CHEMBL23297 | — | — | 1 | 5.09 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 4.92 |
| CHEMBL23846 | — | — | 1 | 4.87 |
| CHEMBL22477 | — | — | 1 | 4.85 |
| CHEMBL22561 | — | — | 1 | 4.83 |
| CHEMBL283515 | — | — | 1 | 4.72 |
| CHEMBL279914 | — | — | 1 | 4.39 |
| CHEMBL23153 | — | — | 1 | 4.35 |
| CHEMBL277438 | — | — | 1 | 4.29 |
| CHEMBL22820 | — | — | 1 | - |
| CHEMBL23658 | — | — | 1 | - |
| CHEMBL23054 | — | — | 1 | - |
| CHEMBL278110 | — | — | 1 | - |
| CHEMBL23353 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL283311 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL280378 | EPIROPRIM | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL23960 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL23297 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL23846 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL22477 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL22561 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL283515 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL279914 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL23153 | — | IC50 | = | 44800.0 | nM | 4.35 |
| CHEMBL277438 | — | IC50 | = | 50900.0 | nM | 4.29 |
| CHEMBL22820 | — | IC50 | > | 26000.0 | nM | - |
| CHEMBL23658 | — | IC50 | > | 31300.0 | nM | - |
| CHEMBL23054 | — | IC50 | > | 27000.0 | nM | - |
| CHEMBL278110 | — | IC50 | = | 284000.0 | nM | - |
| CHEMBL23353 | — | IC50 | > | 12000.0 | nM | - |