Assay Detail
Binding
CHEMBL815678
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In vitro inhibitory activity against thymidylate synthase partially purified from L1210 mouse leukemia cells
34
Total Activities
34
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 antifolates thymidylate synthase inhibitors: lipophilic analogues with modification to the C2-methyl substituent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.68 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348765 | — | — | 1 | 8.00 |
| CHEMBL159593 | — | — | 1 | 7.70 |
| CHEMBL161641 | — | — | 1 | 7.55 |
| CHEMBL268453 | — | — | 1 | 7.36 |
| CHEMBL25889 | — | — | 1 | 7.30 |
| CHEMBL444797 | — | — | 1 | 7.25 |
| CHEMBL159803 | — | — | 1 | 7.14 |
| CHEMBL162891 | — | — | 1 | 7.10 |
| CHEMBL162349 | — | — | 1 | 7.08 |
| CHEMBL159501 | — | — | 1 | 7.00 |
| CHEMBL349448 | — | — | 1 | 7.00 |
| CHEMBL159591 | — | — | 1 | 6.96 |
| CHEMBL161033 | — | — | 1 | 6.96 |
| CHEMBL6325 | — | — | 1 | 6.96 |
| CHEMBL159642 | — | — | 1 | 6.85 |
| CHEMBL159584 | — | — | 1 | 6.80 |
| CHEMBL351864 | — | — | 1 | 6.75 |
| CHEMBL159655 | — | — | 1 | 6.70 |
| CHEMBL161642 | — | — | 1 | 6.62 |
| CHEMBL164315 | — | — | 1 | 6.52 |
| CHEMBL435856 | — | — | 1 | 6.42 |
| CHEMBL162297 | — | — | 1 | 6.42 |
| CHEMBL159633 | — | — | 1 | 6.32 |
| CHEMBL163990 | — | — | 1 | 6.22 |
| CHEMBL423243 | — | — | 1 | 6.21 |
| CHEMBL349365 | — | — | 1 | 6.19 |
| CHEMBL234704 | — | — | 1 | 6.09 |
| CHEMBL158807 | — | — | 1 | 6.08 |
| CHEMBL161081 | — | — | 1 | 6.05 |
| CHEMBL351599 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348765 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL159593 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL161641 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL268453 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL25889 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL444797 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL159803 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL162891 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL162349 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL159501 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL349448 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL159591 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL161033 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL6325 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL159642 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL159584 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL351864 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL159655 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL161642 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL164315 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL435856 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL162297 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL159633 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL163990 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL423243 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL349365 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL234704 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL158807 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL161081 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL351599 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL349196 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL161349 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL159227 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL161049 | — | IC50 | > | 1700.0 | nM | - |