Assay Detail
Binding
CHEMBL669644
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Compound was tested for its ability to inhibit purified dihydrofolate reductase(DHFR) from L1210/R81 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | L1210 ( R81) |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Methotrexate analogues. 26. Inhibition of dihydrofolate reductase and folylpolyglutamate synthetase activity and in vitro tumor cell growth by methotrexate and aminopterin analogues containing a basic amino acid side chain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.10 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376180 | AMINOPTERIN | 2.0 | 1 | 7.46 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.46 |
| CHEMBL418165 | — | — | 1 | 7.19 |
| CHEMBL280864 | — | — | 1 | 7.14 |
| CHEMBL158970 | — | — | 1 | 6.92 |
| CHEMBL36083 | — | — | 1 | 6.80 |
| CHEMBL158478 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376180 | AMINOPTERIN | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL418165 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL280864 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL158970 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL36083 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL158478 | — | IC50 | = | 180.0 | nM | 6.75 |