Assay Detail
Binding
CHEMBL665434
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Inhibition of dihydrofolate reductase from rat liver.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of 2,4-diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase and as antiopportunistic infection and antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.59 | 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 |
| CHEMBL32113 | — | — | 1 | 7.24 |
| CHEMBL147828 | — | — | 1 | 6.75 |
| CHEMBL149099 | — | — | 1 | 6.57 |
| CHEMBL142741 | — | — | 1 | 6.55 |
| CHEMBL147870 | — | — | 1 | 6.32 |
| CHEMBL149301 | — | — | 1 | 6.25 |
| CHEMBL22924 | — | — | 1 | 6.22 |
| CHEMBL356279 | — | — | 1 | 6.10 |
| CHEMBL23288 | — | — | 1 | 5.72 |
| CHEMBL358003 | — | — | 1 | 5.64 |
| CHEMBL358351 | — | — | 1 | 5.34 |
| CHEMBL146039 | — | — | 1 | 5.31 |
| CHEMBL424135 | — | — | 1 | 5.30 |
| CHEMBL145979 | — | — | 1 | 5.16 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
| CHEMBL146622 | — | — | 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 |
| CHEMBL32113 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL147828 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL149099 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL142741 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL147870 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL149301 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL22924 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL356279 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL23288 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL358003 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL358351 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL146039 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL424135 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL145979 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 133000.0 | nM | - |
| CHEMBL146622 | — | IC50 | = | 395000.0 | nM | - |