Assay Detail
Binding
CHEMBL812284
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Tested for inhibition of topoisomerase II isolated from HeLa cells by DNA-cleavage assay
24
Total Activities
24
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
Mammalian topoisomerase II inhibitory activity of 1-cyclopropyl-6,8- difluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolinecarb oxylic acid and related derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 5.02 | 6.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL43 | AMSACRINE | 4.0 | 1 | 6.14 |
| CHEMBL44657 | ETOPOSIDE | 4.0 | 1 | 6.09 |
| CHEMBL96510 | — | — | 1 | 5.92 |
| CHEMBL329385 | — | — | 1 | 5.21 |
| CHEMBL8179 | WIN-57294 | — | 1 | 5.12 |
| CHEMBL441631 | — | — | 1 | 4.89 |
| CHEMBL97087 | — | — | 1 | 4.80 |
| CHEMBL94506 | — | — | 1 | 4.80 |
| CHEMBL414022 | — | — | 1 | 4.77 |
| CHEMBL433389 | — | — | 1 | 4.77 |
| CHEMBL97315 | — | — | 1 | 4.28 |
| CHEMBL327663 | — | — | 1 | 4.28 |
| CHEMBL419703 | — | — | 1 | 4.13 |
| CHEMBL319939 | — | — | 1 | - |
| CHEMBL328719 | — | — | 1 | - |
| CHEMBL97638 | — | — | 1 | - |
| CHEMBL94321 | — | — | 1 | - |
| CHEMBL15464 | — | — | 1 | - |
| CHEMBL544553 | — | — | 1 | - |
| CHEMBL94671 | — | — | 1 | - |
| CHEMBL96509 | — | — | 1 | - |
| CHEMBL47255 | — | — | 1 | - |
| CHEMBL96705 | — | — | 1 | - |
| CHEMBL319529 | — | — | 1 | - |
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 |
| CHEMBL96510 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL329385 | — | EC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL8179 | WIN-57294 | EC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL441631 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL97087 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL94506 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL414022 | — | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL433389 | — | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL97315 | — | EC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL327663 | — | EC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL419703 | — | EC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL319939 | — | EC50 | > | 530000.0 | nM | - |
| CHEMBL328719 | — | EC50 | > | 430000.0 | nM | - |
| CHEMBL97638 | — | EC50 | > | 240000.0 | nM | - |
| CHEMBL94321 | — | EC50 | > | 300000.0 | nM | - |
| CHEMBL15464 | — | EC50 | = | 340000.0 | nM | - |
| CHEMBL544553 | — | EC50 | > | 140000.0 | nM | - |
| CHEMBL94671 | — | EC50 | = | 110000.0 | nM | - |
| CHEMBL96509 | — | EC50 | > | 420000.0 | nM | - |
| CHEMBL47255 | — | EC50 | = | 150000.0 | nM | - |
| CHEMBL96705 | — | EC50 | > | 260000.0 | nM | - |
| CHEMBL319529 | — | EC50 | > | 220000.0 | nM | - |