Assay Detail
Binding
CHEMBL668095
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Inhibitory concentration against Dihydrofolate reductase from rat liver
11
Total Activities
11
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
Design, synthesis, and biological evaluation of 2,4-diamino-5-methyl-6-substituted-pyrrolo[2,3-d]pyrimidines as dihydrofolate reductase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.42 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL123984 | — | — | 1 | 5.69 |
| CHEMBL331314 | — | — | 1 | 5.63 |
| CHEMBL122998 | — | — | 1 | 5.34 |
| CHEMBL331986 | — | — | 1 | 5.11 |
| CHEMBL283311 | — | — | 1 | 4.91 |
| CHEMBL420172 | — | — | 1 | 4.72 |
| CHEMBL123892 | — | — | 1 | 4.50 |
| CHEMBL334198 | — | — | 1 | 4.32 |
| CHEMBL331456 | — | — | 1 | - |
| CHEMBL331292 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL123984 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL331314 | — | IC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL122998 | — | IC50 | = | 4570.0 | nM | 5.34 |
| CHEMBL331986 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL283311 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL420172 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL123892 | — | IC50 | = | 31300.0 | nM | 4.50 |
| CHEMBL334198 | — | IC50 | = | 47700.0 | nM | 4.32 |
| CHEMBL331456 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL331292 | — | IC50 | = | 180000.0 | nM | - |