Assay Detail
Binding
CHEMBL847692
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Inhibitory activity in a cell-free assay of DNA cleavage mediated by purified HeLa cell topoisomerase II.
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HeLa |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Potent mammalian topoisomerase II inhibitors: 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-substituted-quinolines
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 31 | 5.27 | 6.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL43 | AMSACRINE | 4.0 | 1 | 6.14 |
| CHEMBL44657 | ETOPOSIDE | 4.0 | 1 | 6.09 |
| CHEMBL133780 | — | — | 1 | 6.01 |
| CHEMBL129840 | — | — | 1 | 5.85 |
| CHEMBL422791 | — | — | 1 | 5.80 |
| CHEMBL337666 | — | — | 1 | 5.77 |
| CHEMBL422265 | — | — | 1 | 5.72 |
| CHEMBL334608 | — | — | 1 | 5.64 |
| CHEMBL132656 | — | — | 1 | 5.62 |
| CHEMBL449700 | — | — | 1 | 5.58 |
| CHEMBL335683 | — | — | 1 | 5.57 |
| CHEMBL262982 | — | — | 1 | 5.51 |
| CHEMBL336767 | — | — | 1 | 5.50 |
| CHEMBL130706 | — | — | 1 | 5.44 |
| CHEMBL130047 | — | — | 1 | 5.42 |
| CHEMBL130547 | — | — | 1 | 5.40 |
| CHEMBL339781 | — | — | 1 | 5.32 |
| CHEMBL131208 | — | — | 1 | 5.26 |
| CHEMBL130889 | — | — | 1 | 5.20 |
| CHEMBL128466 | — | — | 1 | 5.12 |
| CHEMBL8179 | WIN-57294 | — | 1 | 5.12 |
| CHEMBL130538 | — | — | 1 | 5.03 |
| CHEMBL130097 | — | — | 1 | 4.92 |
| CHEMBL129892 | — | — | 1 | 4.85 |
| CHEMBL130662 | — | — | 1 | 4.80 |
| CHEMBL414022 | — | — | 1 | 4.77 |
| CHEMBL130838 | — | — | 1 | 4.70 |
| CHEMBL359932 | — | — | 1 | 4.68 |
| CHEMBL130368 | — | — | 1 | 4.35 |
| CHEMBL130604 | — | — | 1 | 4.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL43 | AMSACRINE | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL44657 | ETOPOSIDE | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL133780 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL129840 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL422791 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL337666 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL422265 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL334608 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL132656 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL449700 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL335683 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL262982 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL336767 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL130706 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL130047 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL130547 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL339781 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL131208 | — | EC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL130889 | — | EC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL128466 | — | EC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL8179 | WIN-57294 | EC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL130538 | — | EC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL130097 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL129892 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL130662 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL414022 | — | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL130838 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL359932 | — | EC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL130368 | — | EC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL130604 | — | EC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL132213 | — | EC50 | = | 92000.0 | nM | 4.04 |