Assay Detail
Binding
CHEMBL665440
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Inhibitory activity against DHFR (Dihydrofolate reductase) from Rat liver
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.37 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL144839 | — | — | 1 | 7.57 |
| CHEMBL423200 | — | — | 1 | 7.26 |
| CHEMBL144200 | — | — | 1 | 6.70 |
| CHEMBL424113 | — | — | 1 | 5.40 |
| CHEMBL301769 | — | — | 1 | 5.36 |
| CHEMBL342086 | — | — | 1 | 5.29 |
| CHEMBL423381 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL144839 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL423200 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL144200 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL424113 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL301769 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL342086 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL423381 | — | IC50 | = | 13000.0 | nM | 4.89 |