Assay Detail
Binding
CHEMBL815659
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Inhibitory activity against thymidylate synthase isolated from L1210 leukemia cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | L1210 |
| 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 | 26 | 5.97 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL422395 | — | — | 1 | 7.85 |
| CHEMBL305253 | — | — | 1 | 7.48 |
| CHEMBL39674 | — | — | 1 | 7.01 |
| CHEMBL343140 | — | — | 1 | 6.89 |
| CHEMBL36866 | — | — | 1 | 6.82 |
| CHEMBL37061 | — | — | 1 | 6.72 |
| CHEMBL74659 | — | — | 1 | 6.70 |
| CHEMBL138870 | — | — | 1 | 6.66 |
| CHEMBL423123 | — | — | 1 | 6.26 |
| CHEMBL304397 | — | — | 1 | 6.22 |
| CHEMBL80135 | — | — | 1 | 6.16 |
| CHEMBL36739 | — | — | 1 | 5.89 |
| CHEMBL35936 | — | — | 1 | 5.66 |
| CHEMBL141576 | — | — | 1 | 5.50 |
| CHEMBL23977 | DIDEAZAFOLATE | — | 1 | 5.47 |
| CHEMBL39851 | — | — | 1 | 5.40 |
| CHEMBL141648 | — | — | 1 | 5.36 |
| CHEMBL305177 | — | — | 1 | 5.30 |
| CHEMBL442217 | — | — | 1 | 5.21 |
| CHEMBL141857 | — | — | 1 | 5.07 |
| CHEMBL140448 | — | — | 1 | 5.01 |
| CHEMBL77065 | — | — | 1 | 4.96 |
| CHEMBL139551 | — | — | 1 | 4.92 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 4.70 |
| CHEMBL303654 | — | — | 1 | - |
| CHEMBL69713 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL422395 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL305253 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL39674 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL343140 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL36866 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL37061 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL74659 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL138870 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL423123 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL304397 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL80135 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL36739 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL35936 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL141576 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL23977 | DIDEAZAFOLATE | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL39851 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL141648 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL305177 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL442217 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL141857 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL140448 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL77065 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL139551 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL303654 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL69713 | — | IC50 | > | 10000.0 | nM | - |