Assay Detail
Functional
CHEMBL864040
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Inhibition of telomerase activity from human A2780 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A2780 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Trisubstituted acridines as G-quadruplex telomere targeting agents. Effects of extensions of the 3,6- and 9-side chains on quadruplex binding, telomerase activity, and cell proliferation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 6.45 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL201766 | — | — | 1 | 7.17 |
| CHEMBL201697 | — | — | 1 | 7.00 |
| CHEMBL336434 | — | — | 1 | 6.95 |
| CHEMBL202769 | — | — | 1 | 6.93 |
| CHEMBL383282 | — | — | 1 | 6.84 |
| CHEMBL264477 | — | — | 1 | 6.78 |
| CHEMBL202717 | — | — | 1 | 6.59 |
| CHEMBL203366 | — | — | 1 | 6.49 |
| CHEMBL202167 | — | — | 1 | 5.71 |
| CHEMBL202820 | — | — | 1 | 5.28 |
| CHEMBL202562 | — | — | 1 | 5.16 |
| CHEMBL381966 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL201766 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL201697 | — | EC50 | = | 99.0 | nM | 7.00 |
| CHEMBL336434 | — | EC50 | = | 113.0 | nM | 6.95 |
| CHEMBL202769 | — | EC50 | = | 117.0 | nM | 6.93 |
| CHEMBL383282 | — | EC50 | = | 146.0 | nM | 6.84 |
| CHEMBL264477 | — | EC50 | = | 167.0 | nM | 6.78 |
| CHEMBL202717 | — | EC50 | = | 255.0 | nM | 6.59 |
| CHEMBL203366 | — | EC50 | = | 326.0 | nM | 6.49 |
| CHEMBL202167 | — | EC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL202820 | — | EC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL202562 | — | EC50 | = | 6910.0 | nM | 5.16 |
| CHEMBL381966 | — | EC50 | > | 20000.0 | nM | - |