Assay Detail
Binding
CHEMBL665455
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Inhibition of rat liver dihydrofolate reductase
13
Total Activities
13
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 of 5-methyl-5-deaza nonclassical antifolates as inhibitors of dihydrofolate reductases and as potential antipneumocystis, antitoxoplasma, and antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.52 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.82 |
| CHEMBL23532 | — | — | 1 | 8.68 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL50514 | — | — | 1 | 8.12 |
| CHEMBL420224 | — | — | 1 | 7.48 |
| CHEMBL82924 | — | — | 1 | 7.44 |
| CHEMBL82975 | — | — | 1 | 7.38 |
| CHEMBL81820 | — | — | 1 | 7.28 |
| CHEMBL115788 | — | — | 1 | 6.96 |
| CHEMBL334271 | — | — | 1 | 6.60 |
| CHEMBL421053 | — | — | 1 | 5.43 |
| CHEMBL114668 | — | — | 1 | - |
| CHEMBL117172 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL23532 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL50514 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL420224 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL82924 | — | IC50 | = | 36.3 | nM | 7.44 |
| CHEMBL82975 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL81820 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL115788 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL334271 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL421053 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL114668 | — | IC50 | > | 2600.0 | nM | - |
| CHEMBL117172 | — | IC50 | > | 1200.0 | nM | - |