Assay Detail
Binding
CHEMBL821265
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Inhibition of Thymidylate Synthase(TS) from mouse L1210 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | L1210 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Folate-based inhibitors of thymidylate synthase: synthesis and antitumor activity of gamma-linked sterically hindered dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.26 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL30179 | — | — | 1 | 9.68 |
| CHEMBL35926 | — | — | 1 | 9.46 |
| CHEMBL37106 | — | — | 1 | 8.96 |
| CHEMBL288666 | — | — | 1 | 8.70 |
| CHEMBL291084 | — | — | 1 | 8.59 |
| CHEMBL289749 | — | — | 1 | 8.52 |
| CHEMBL264609 | — | — | 1 | 8.40 |
| CHEMBL36433 | — | — | 1 | 8.09 |
| CHEMBL36721 | — | — | 1 | 8.07 |
| CHEMBL288615 | — | — | 1 | 7.96 |
| CHEMBL287693 | — | — | 1 | 7.75 |
| CHEMBL36426 | — | — | 1 | 7.64 |
| CHEMBL284613 | — | — | 1 | 7.46 |
| CHEMBL34857 | — | — | 1 | 7.38 |
| CHEMBL35941 | — | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL30179 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL35926 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL37106 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL288666 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL291084 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL289749 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL264609 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL36433 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL36721 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL288615 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL287693 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL36426 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL284613 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL34857 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL35941 | — | Ki | = | 50.0 | nM | 7.30 |