Assay Detail
Binding
CHEMBL820613
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Thymidylate synthase activity in L1210 cells
20
Total Activities
19
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: gamma-linked L-D, D-D, and D-L dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.23 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL170933 | — | — | 1 | 9.40 |
| CHEMBL349432 | — | — | 1 | 9.25 |
| CHEMBL354785 | — | — | 1 | 8.72 |
| CHEMBL353066 | — | — | 1 | 8.72 |
| CHEMBL168952 | — | — | 1 | 8.70 |
| CHEMBL355543 | — | — | 1 | 8.70 |
| CHEMBL170494 | — | — | 1 | 8.70 |
| CHEMBL168970 | — | — | 2 | 8.38 |
| CHEMBL170789 | — | — | 1 | 8.34 |
| CHEMBL367732 | — | — | 1 | 8.34 |
| CHEMBL263325 | — | — | 1 | 8.06 |
| CHEMBL170975 | — | — | 1 | 7.92 |
| CHEMBL168450 | — | — | 1 | 7.89 |
| CHEMBL424541 | — | — | 1 | 7.77 |
| CHEMBL352327 | — | — | 1 | 7.75 |
| CHEMBL168553 | — | — | 1 | 7.57 |
| CHEMBL352357 | — | — | 1 | 7.52 |
| CHEMBL349488 | — | — | 1 | 7.47 |
| CHEMBL169540 | — | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL170933 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL349432 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL354785 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL353066 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL168952 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL355543 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL170494 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL168970 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL367732 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL170789 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL263325 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL168970 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL170975 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL168450 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL424541 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL352327 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL168553 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL352357 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL349488 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL169540 | — | IC50 | = | 37.0 | nM | 7.43 |