Assay Detail
Binding
CHEMBL1020204
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DNA topoisomerase 1-mediated DNA cleavage assessed as relaxation of supercoiled pBR322 plasmid DNA after 15 mins by densitometer
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological activities of topoisomerase I inhibitors, 6-arylmethylamino analogues of edotecarin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 7.52 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL474561 | — | — | 1 | 8.48 |
| CHEMBL507686 | — | — | 1 | 7.92 |
| CHEMBL503051 | — | — | 1 | 7.80 |
| CHEMBL447826 | — | — | 1 | 7.77 |
| CHEMBL478720 | — | — | 1 | 7.72 |
| CHEMBL452445 | — | — | 1 | 7.70 |
| CHEMBL505815 | — | — | 1 | 7.70 |
| CHEMBL455328 | — | — | 1 | 7.66 |
| CHEMBL449831 | — | — | 1 | 7.66 |
| CHEMBL446276 | — | — | 1 | 7.66 |
| CHEMBL510006 | — | — | 1 | 7.64 |
| CHEMBL454734 | — | — | 1 | 7.60 |
| CHEMBL502679 | — | — | 1 | 7.60 |
| CHEMBL507295 | — | — | 1 | 7.57 |
| CHEMBL509544 | — | — | 1 | 7.54 |
| CHEMBL500059 | — | — | 1 | 7.52 |
| CHEMBL503252 | — | — | 1 | 7.52 |
| CHEMBL475683 | — | — | 1 | 7.52 |
| CHEMBL450991 | — | — | 1 | 7.52 |
| CHEMBL448760 | — | — | 1 | 7.52 |
| CHEMBL507006 | — | — | 1 | 7.51 |
| CHEMBL117315 | — | — | 1 | 7.47 |
| CHEMBL506902 | — | — | 1 | 7.46 |
| CHEMBL508108 | — | — | 1 | 7.46 |
| CHEMBL499795 | — | — | 1 | 7.42 |
| CHEMBL435191 | EDOTECARIN | 3.0 | 1 | 7.00 |
| CHEMBL463738 | — | — | 1 | 6.52 |
| CHEMBL499103 | — | — | 1 | 6.10 |
| CHEMBL455326 | — | — | 1 | - |
| CHEMBL447330 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL474561 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL507686 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL503051 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL447826 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL478720 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL452445 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL505815 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL455328 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL449831 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL446276 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL510006 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL454734 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL502679 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL507295 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL509544 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL500059 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL503252 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL475683 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL450991 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL448760 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL507006 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL117315 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL506902 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL508108 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL499795 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL435191 | EDOTECARIN | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL463738 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL499103 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL455326 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL447330 | — | EC50 | - | — | - |