Assay Detail
Binding
CHEMBL821264
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Inhibition of thymidylate synthase, partially purified from L1210 mouse leukemia cells overexpressing TS
17
Total Activities
17
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
Syntheses and thymidylate synthase inhibitory activity of the poly-gamma-glutamyl conjugates of N-[5-[N-(3,4-dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl)-N-methylamino ]-2-thenoyl]-L-glutamic acid (ICI D1694) and other quinazoline antifolates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.50 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1202139 | — | — | 1 | 9.57 |
| CHEMBL264807 | — | — | 1 | 9.40 |
| CHEMBL1202137 | — | — | 1 | 9.40 |
| CHEMBL171226 | — | — | 1 | 9.23 |
| CHEMBL1202138 | — | — | 1 | 9.20 |
| CHEMBL1202140 | — | — | 1 | 9.01 |
| CHEMBL436448 | — | — | 1 | 9.00 |
| CHEMBL355543 | — | — | 1 | 8.96 |
| CHEMBL405513 | — | — | 1 | 8.43 |
| CHEMBL268593 | — | — | 1 | 8.42 |
| CHEMBL172160 | — | — | 1 | 8.33 |
| CHEMBL355321 | — | — | 1 | 8.12 |
| CHEMBL169981 | — | — | 1 | 7.98 |
| CHEMBL353302 | — | — | 1 | 7.62 |
| CHEMBL434209 | — | — | 1 | 7.50 |
| CHEMBL96367 | — | — | 1 | 7.20 |
| CHEMBL103059 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1202139 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL264807 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1202137 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL171226 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL1202138 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL1202140 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL436448 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL355543 | — | Ki | = | 1.11 | nM | 8.96 |
| CHEMBL405513 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL268593 | — | Ki | = | 3.79 | nM | 8.42 |
| CHEMBL172160 | — | Ki | = | 4.69 | nM | 8.33 |
| CHEMBL355321 | — | Ki | = | 7.52 | nM | 8.12 |
| CHEMBL169981 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL353302 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL434209 | — | Ki | = | 31.38 | nM | 7.50 |
| CHEMBL96367 | — | Ki | = | 63.7 | nM | 7.20 |
| CHEMBL103059 | — | Ki | = | 63.68 | nM | 7.20 |