Assay Detail
Binding
CHEMBL844165
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Time-independent inhibition of thymidylate synthase from FdUrd-resistant L1210 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | L1210 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
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 | 11 | 5.74 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL886 | 5-FLUORODEOXYURIDYLATE | — | 1 | 7.52 |
| CHEMBL1236538 | — | — | 1 | 6.82 |
| CHEMBL1160593 | — | — | 1 | 6.34 |
| CHEMBL1160818 | — | — | 1 | 6.05 |
| CHEMBL1161226 | — | — | 1 | 5.85 |
| CHEMBL1161224 | — | — | 1 | 5.66 |
| CHEMBL1161225 | — | — | 1 | 5.24 |
| CHEMBL1160594 | — | — | 1 | 5.16 |
| CHEMBL1161232 | — | — | 1 | 5.08 |
| CHEMBL1161227 | — | — | 1 | 5.03 |
| CHEMBL1161231 | — | — | 1 | 4.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL886 | 5-FLUORODEOXYURIDYLATE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1236538 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL1160593 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL1160818 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL1161226 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL1161224 | — | Ki | = | 2180.0 | nM | 5.66 |
| CHEMBL1161225 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL1160594 | — | Ki | = | 6990.0 | nM | 5.16 |
| CHEMBL1161232 | — | Ki | = | 8400.0 | nM | 5.08 |
| CHEMBL1161227 | — | Ki | = | 9300.0 | nM | 5.03 |
| CHEMBL1161231 | — | Ki | = | 36600.0 | nM | 4.44 |