Assay Detail
Binding
CHEMBL669446
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Inhibitory activity against dihydrofolate reductase (DHFR) obtained from human WIL2 cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | WIL2 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Inhibition of murine thymidylate synthase and human dihydrofolate reductase by 5,8-dideaza analogues of folic acid and aminopterin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.34 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL37061 | — | — | 1 | 8.42 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.42 |
| CHEMBL304397 | — | — | 1 | 8.41 |
| CHEMBL36866 | — | — | 1 | 8.39 |
| CHEMBL305177 | — | — | 1 | 8.35 |
| CHEMBL305253 | — | — | 1 | 8.34 |
| CHEMBL141648 | — | — | 1 | 8.28 |
| CHEMBL141576 | — | — | 1 | 8.27 |
| CHEMBL303654 | — | — | 1 | 8.24 |
| CHEMBL69713 | — | — | 1 | 8.24 |
| CHEMBL423123 | — | — | 1 | 8.07 |
| CHEMBL140448 | — | — | 1 | 7.96 |
| CHEMBL23977 | DIDEAZAFOLATE | — | 1 | 7.47 |
| CHEMBL343140 | — | — | 1 | 7.08 |
| CHEMBL39851 | — | — | 1 | 7.00 |
| CHEMBL36739 | — | — | 1 | 6.96 |
| CHEMBL139551 | — | — | 1 | 6.77 |
| CHEMBL77065 | — | — | 1 | 6.55 |
| CHEMBL74659 | — | — | 1 | 6.52 |
| CHEMBL138870 | — | — | 1 | 6.48 |
| CHEMBL35936 | — | — | 1 | 6.34 |
| CHEMBL422395 | — | — | 1 | 6.04 |
| CHEMBL442217 | — | — | 1 | 5.85 |
| CHEMBL141857 | — | — | 1 | 5.52 |
| CHEMBL80135 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL37061 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL304397 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL36866 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL305177 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL305253 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL141648 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL141576 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL303654 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL69713 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL423123 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL140448 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL23977 | DIDEAZAFOLATE | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL343140 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL39851 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL36739 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL139551 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL77065 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL74659 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL138870 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL35936 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL422395 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL442217 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL141857 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL80135 | — | IC50 | = | 3200.0 | nM | 5.50 |