Assay Detail
Binding
CHEMBL815661
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Inhibition of thymidylate synthase purified from mouse L1210 leukemia cells that overproduce thymidylate synthase (TS)
30
Total Activities
30
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 | 30 | 6.60 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6271 | — | — | 1 | 8.36 |
| CHEMBL414012 | — | — | 1 | 8.05 |
| CHEMBL6636 | — | — | 1 | 7.62 |
| CHEMBL266956 | — | — | 1 | 7.47 |
| CHEMBL6676 | — | — | 1 | 7.40 |
| CHEMBL6788 | — | — | 1 | 7.38 |
| CHEMBL268629 | — | — | 1 | 7.38 |
| CHEMBL268453 | — | — | 1 | 7.36 |
| CHEMBL6663 | — | — | 1 | 7.24 |
| CHEMBL267832 | — | — | 1 | 7.24 |
| CHEMBL266509 | — | — | 1 | 7.17 |
| CHEMBL6325 | — | — | 1 | 6.96 |
| CHEMBL266508 | — | — | 1 | 6.82 |
| CHEMBL415104 | — | — | 1 | 6.77 |
| CHEMBL6850 | — | — | 1 | 6.57 |
| CHEMBL268100 | — | — | 1 | 6.55 |
| CHEMBL6775 | — | — | 1 | 6.50 |
| CHEMBL6357 | — | — | 1 | 6.35 |
| CHEMBL6560 | — | — | 1 | 6.28 |
| CHEMBL266065 | — | — | 1 | 6.28 |
| CHEMBL6829 | — | — | 1 | 6.14 |
| CHEMBL6496 | — | — | 1 | 6.07 |
| CHEMBL6590 | — | — | 1 | 5.86 |
| CHEMBL264097 | — | — | 1 | 5.85 |
| CHEMBL6317 | — | — | 1 | 5.84 |
| CHEMBL415105 | — | — | 1 | 5.74 |
| CHEMBL265410 | — | — | 1 | 5.65 |
| CHEMBL6498 | — | — | 1 | 5.38 |
| CHEMBL268854 | — | — | 1 | 5.11 |
| CHEMBL6307 | — | — | 1 | 4.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6271 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL414012 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL6636 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL266956 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL6676 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL6788 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL268629 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL268453 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL6663 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL267832 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL266509 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL6325 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL266508 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL415104 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL6850 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL268100 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL6775 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL6357 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL6560 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL266065 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL6829 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL6496 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL6590 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL264097 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL6317 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL415105 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL265410 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL6498 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL268854 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL6307 | — | IC50 | = | 22900.0 | nM | 4.64 |