Assay Detail
Binding
CHEMBL669448
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit purified Dihydrofolate reductase from human leukemic lymphoblasts was determined spectrophotometrically at 340 nM.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Analogues of methotrexate and aminopterin with gamma-methylene and gamma-cyano substitution of the glutamate side chain: synthesis and in vitro biological activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.37 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.60 |
| CHEMBL376180 | AMINOPTERIN | 2.0 | 1 | 7.60 |
| CHEMBL65616 | — | — | 1 | 7.36 |
| CHEMBL65620 | — | — | 1 | 7.24 |
| CHEMBL65711 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL376180 | AMINOPTERIN | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL65616 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL65620 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL65711 | — | IC50 | = | 88.0 | nM | 7.06 |