Assay Detail
Binding
CHEMBL665445
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Inhibitory activity against rat liver Dihydrofolate reductase
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 6.03 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.82 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL341703 | — | — | 1 | 6.29 |
| CHEMBL164845 | — | — | 1 | 5.82 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 5.64 |
| CHEMBL441298 | — | — | 1 | 5.43 |
| CHEMBL349149 | — | — | 1 | 5.39 |
| CHEMBL162270 | — | — | 1 | 4.28 |
| CHEMBL434097 | — | — | 1 | 4.08 |
| CHEMBL162312 | — | — | 1 | - |
| CHEMBL350730 | — | — | 1 | - |
| CHEMBL355151 | — | — | 1 | - |
| CHEMBL165955 | — | — | 1 | - |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL341703 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL164845 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL441298 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL349149 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL162270 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL434097 | — | IC50 | = | 84000.0 | nM | 4.08 |
| CHEMBL162312 | — | IC50 | > | 18000.0 | nM | - |
| CHEMBL350730 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL355151 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL165955 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 130000.0 | nM | - |