Assay Detail
Binding
CHEMBL664185
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Inhibitory activity against Dihydrofolate reductase from Pneumocystis carinii was evaluated using 90 uM dihydrofolic acid as substrate
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Pneumocystis carinii |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Nonclassical 2,4-diamino-5-aryl-6-ethylpyrimidine antifolates: activity as inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.37 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.89 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 7.51 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 7.38 |
| CHEMBL103086 | — | — | 1 | 7.00 |
| CHEMBL102850 | — | — | 1 | 6.57 |
| CHEMBL103981 | — | — | 1 | 6.57 |
| CHEMBL102447 | — | — | 1 | 6.35 |
| CHEMBL102418 | — | — | 1 | 6.34 |
| CHEMBL102996 | — | — | 1 | 6.34 |
| CHEMBL323359 | — | — | 1 | 6.28 |
| CHEMBL104020 | — | — | 1 | 6.24 |
| CHEMBL59530 | — | — | 1 | 6.07 |
| CHEMBL105526 | — | — | 1 | 6.03 |
| CHEMBL103971 | — | — | 1 | 6.02 |
| CHEMBL81294 | — | — | 1 | 5.99 |
| CHEMBL102967 | — | — | 1 | 5.89 |
| CHEMBL56170 | — | — | 1 | 5.80 |
| CHEMBL103558 | — | — | 1 | 5.66 |
| CHEMBL280378 | EPIROPRIM | 2.0 | 1 | 5.58 |
| CHEMBL3142796 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL103086 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL102850 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL103981 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL102447 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL102418 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL102996 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL323359 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL104020 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL59530 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL105526 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL103971 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL81294 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL102967 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL56170 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL103558 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL280378 | EPIROPRIM | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3142796 | — | IC50 | = | 12000.0 | nM | 4.92 |