Assay Detail
Binding
CHEMBL666701
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Dihydrofolate Reductase of Rat Liver.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of nonclassical 2,4-diamino-5-methylpyrido[2,3-d]pyrimidines with novel side chain substituents as potential inhibitors of dihydrofolate reductases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.72 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.82 |
| CHEMBL23532 | — | — | 1 | 8.52 |
| CHEMBL23021 | — | — | 1 | 6.89 |
| CHEMBL147886 | — | — | 1 | 6.89 |
| CHEMBL359454 | — | — | 1 | 6.82 |
| CHEMBL146438 | — | — | 1 | 6.77 |
| CHEMBL144563 | — | — | 1 | 6.77 |
| CHEMBL423560 | — | — | 1 | 6.64 |
| CHEMBL435479 | — | — | 1 | 6.64 |
| CHEMBL357629 | — | — | 1 | 6.36 |
| CHEMBL358297 | — | — | 1 | 6.33 |
| CHEMBL356722 | — | — | 1 | 5.46 |
| CHEMBL280378 | EPIROPRIM | 2.0 | 1 | 4.48 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL23532 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL23021 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL147886 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL359454 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL146438 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL144563 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL423560 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL435479 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL357629 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL358297 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL356722 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL280378 | EPIROPRIM | IC50 | = | 33200.0 | nM | 4.48 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 133000.0 | nM | - |