Assay Detail
Binding
CHEMBL664182
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Inhibitory activity against dihydrofolate reductase (DHFR) from Pneumocystis carinii
24
Total Activities
24
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
6-Substituted 2,4-diaminopyrido[3,2-d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver, Pneumocystis carinii, and Toxoplasma gondii and as antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.82 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL337603 | — | — | 1 | 8.64 |
| CHEMBL139485 | — | — | 1 | 7.68 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 7.51 |
| CHEMBL141698 | — | — | 1 | 7.47 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 7.38 |
| CHEMBL137981 | — | — | 1 | 7.07 |
| CHEMBL140940 | — | — | 1 | 7.00 |
| CHEMBL141160 | — | — | 1 | 6.66 |
| CHEMBL137844 | — | — | 1 | 6.16 |
| CHEMBL142081 | — | — | 1 | 5.66 |
| CHEMBL140597 | — | — | 1 | 5.57 |
| CHEMBL337746 | — | — | 1 | 5.50 |
| CHEMBL334456 | — | — | 1 | 5.29 |
| CHEMBL139188 | — | — | 1 | 5.08 |
| CHEMBL140705 | — | — | 1 | 5.06 |
| CHEMBL342654 | — | — | 1 | 4.98 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 4.92 |
| CHEMBL138252 | — | — | 1 | 4.84 |
| CHEMBL138419 | — | — | 1 | 4.82 |
| CHEMBL141260 | — | — | 1 | 4.79 |
| CHEMBL138452 | — | — | 1 | 4.59 |
| CHEMBL141808 | — | — | 1 | 4.53 |
| CHEMBL141585 | — | — | 1 | 4.39 |
| CHEMBL141218 | — | — | 1 | 4.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL337603 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL139485 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL141698 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL137981 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL140940 | — | IC50 | = | 99.5 | nM | 7.00 |
| CHEMBL141160 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL137844 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL142081 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL140597 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL337746 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL334456 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL139188 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL140705 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL342654 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL138252 | — | IC50 | = | 14600.0 | nM | 4.84 |
| CHEMBL138419 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL141260 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL138452 | — | IC50 | = | 25900.0 | nM | 4.59 |
| CHEMBL141808 | — | IC50 | = | 29400.0 | nM | 4.53 |
| CHEMBL141585 | — | IC50 | = | 40400.0 | nM | 4.39 |
| CHEMBL141218 | — | IC50 | = | 90400.0 | nM | 4.04 |