Assay Detail
Binding
CHEMBL1763192
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 4 hrs by liquid scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | L1210 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of unsaturated keto and exomethylene D-arabinopyranonucleoside analogs: novel 5-fluorouracil analogs that target thymidylate synthase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.53 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL917 | FLOXURIDINE | 4.0 | 1 | 9.40 |
| CHEMBL185 | FLUOROURACIL | 4.0 | 1 | 6.66 |
| CHEMBL1762220 | — | — | 1 | 6.08 |
| CHEMBL1762230 | — | — | 1 | 5.44 |
| CHEMBL1762225 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL917 | FLOXURIDINE | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL185 | FLUOROURACIL | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1762220 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL1762230 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1762225 | — | IC50 | = | 8700.0 | nM | 5.06 |