Assay Detail
Binding
CHEMBL815669
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Concentration required to inhibit 50% activity of Thymidylate synthase was determined
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Quinazoline antifolate thymidylate synthase inhibitors: 2'-fluoro-N10-propargyl-5,8-dideazafolic acid and derivatives with modifications in the C2 position.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.36 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL104230 | — | — | 1 | 8.05 |
| CHEMBL389051 | — | — | 1 | 7.70 |
| CHEMBL169981 | — | — | 1 | 7.70 |
| CHEMBL105026 | — | — | 1 | 7.44 |
| CHEMBL434209 | — | — | 1 | 7.30 |
| CHEMBL420280 | — | — | 1 | 7.24 |
| CHEMBL104410 | — | — | 1 | 7.24 |
| CHEMBL265098 | — | — | 1 | 7.17 |
| CHEMBL321977 | — | — | 1 | 7.01 |
| CHEMBL103059 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL104230 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL389051 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL169981 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL105026 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL434209 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL420280 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL104410 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL265098 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL321977 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL103059 | — | IC50 | = | 170.0 | nM | 6.77 |