Assay Detail
Functional
CHEMBL707445
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The compound was tested for inhibition of isolated thymidylate synthase partially purified from L1210 mouse leukemia cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | L1210 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.18 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL126648 | PLEVITREXED | 2.0 | 1 | 9.36 |
| CHEMBL128033 | — | — | 1 | 8.12 |
| CHEMBL434209 | — | — | 1 | 8.00 |
| CHEMBL389051 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL126648 | PLEVITREXED | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL128033 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL434209 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL389051 | — | Ki | = | 60.0 | nM | 7.22 |