Assay Detail
Binding
CHEMBL815660
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Ability to inhibit Thymidylate synthase purified from mouse L1210 leukemia cells that overproduce thymidylate synthase (TS)
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 | Expert |
Publication
Quinazoline antifolate thymidylate synthase inhibitors: replacement of glutamic acid in the C2-methyl series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.95 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6715 | — | — | 1 | 8.22 |
| CHEMBL6436 | — | — | 1 | 8.15 |
| CHEMBL264095 | — | — | 1 | 7.32 |
| CHEMBL265669 | — | — | 1 | 7.05 |
| CHEMBL268151 | — | — | 1 | 7.00 |
| CHEMBL266066 | — | — | 1 | 6.96 |
| CHEMBL6632 | — | — | 1 | 6.94 |
| CHEMBL6639 | — | — | 1 | 6.80 |
| CHEMBL267702 | — | — | 1 | 6.12 |
| CHEMBL269600 | — | — | 1 | 6.11 |
| CHEMBL269342 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6715 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL6436 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL264095 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL265669 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL268151 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL266066 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL6632 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL6639 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL267702 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL269600 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL269342 | — | IC50 | = | 1720.0 | nM | 5.76 |