Assay Detail
Binding
CHEMBL874101
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Time-independent inhibition of thymidylate synthase from parenteral L1210 cells
12
Total Activities
12
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 | Expert |
Publication
5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 5.67 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL886 | 5-FLUORODEOXYURIDYLATE | — | 1 | 7.70 |
| CHEMBL1236538 | — | — | 1 | 6.52 |
| CHEMBL1161226 | — | — | 1 | 6.10 |
| CHEMBL1160593 | — | — | 1 | 5.82 |
| CHEMBL1161227 | — | — | 1 | 5.77 |
| CHEMBL1161224 | — | — | 1 | 5.72 |
| CHEMBL1160818 | — | — | 1 | 5.43 |
| CHEMBL235506 | — | — | 1 | 5.14 |
| CHEMBL1161225 | — | — | 1 | 5.13 |
| CHEMBL1160594 | — | — | 1 | 5.12 |
| CHEMBL1161232 | — | — | 1 | 5.07 |
| CHEMBL1161231 | — | — | 1 | 4.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL886 | 5-FLUORODEOXYURIDYLATE | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1236538 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL1161226 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL1160593 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL1161227 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL1161224 | — | Ki | = | 1910.0 | nM | 5.72 |
| CHEMBL1160818 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL235506 | — | Ki | = | 7300.0 | nM | 5.14 |
| CHEMBL1161225 | — | Ki | = | 7460.0 | nM | 5.13 |
| CHEMBL1160594 | — | Ki | = | 7680.0 | nM | 5.12 |
| CHEMBL1161232 | — | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL1161231 | — | Ki | = | 32100.0 | nM | 4.49 |