Assay Detail
Binding
CHEMBL820615
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Tested for inhibition against thymidylate synthase(TS) which is partially purified from L1210 mouse leukemia cells
22
Total Activities
22
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
The synthesis and thymidylate synthase inhibitory activity of L-gamma-L-linked dipeptide and L-gamma-amide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.70 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL326128 | — | — | 1 | 8.70 |
| CHEMBL320794 | — | — | 1 | 8.70 |
| CHEMBL112185 | — | — | 1 | 8.37 |
| CHEMBL113266 | — | — | 1 | 8.00 |
| CHEMBL109282 | — | — | 1 | 7.96 |
| CHEMBL112573 | — | — | 1 | 7.85 |
| CHEMBL324598 | — | — | 1 | 7.85 |
| CHEMBL112110 | — | — | 1 | 7.85 |
| CHEMBL265308 | — | — | 1 | 7.80 |
| CHEMBL320530 | — | — | 1 | 7.80 |
| CHEMBL263535 | — | — | 1 | 7.77 |
| CHEMBL322747 | — | — | 1 | 7.75 |
| CHEMBL112450 | — | — | 1 | 7.75 |
| CHEMBL320531 | — | — | 1 | 7.70 |
| CHEMBL113601 | — | — | 1 | 7.66 |
| CHEMBL1790836 | — | — | 1 | 7.62 |
| CHEMBL323659 | — | — | 1 | 7.31 |
| CHEMBL324528 | — | — | 1 | 7.19 |
| CHEMBL322140 | — | — | 1 | 7.16 |
| CHEMBL113016 | — | — | 1 | 6.93 |
| CHEMBL112128 | — | — | 1 | 6.82 |
| CHEMBL320977 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL326128 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL320794 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL112185 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL113266 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL109282 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL112573 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL324598 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL112110 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL265308 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL320530 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL263535 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL322747 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL112450 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL320531 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL113601 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1790836 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL323659 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL324528 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL322140 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL113016 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL112128 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL320977 | — | IC50 | = | 170.0 | nM | 6.77 |