Assay Detail
Binding
CHEMBL1020203
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DNA topoisomerase 1 in mouse P388/S cells assessed as formation of topoisomerase 1-DNA complex by proteinase K/SDS method
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | P388/S |
| 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 | 6.55 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL435191 | EDOTECARIN | 3.0 | 1 | 8.82 |
| CHEMBL505815 | — | — | 1 | 7.64 |
| CHEMBL503051 | — | — | 1 | 7.62 |
| CHEMBL474561 | — | — | 1 | 7.14 |
| CHEMBL454734 | — | — | 1 | 7.10 |
| CHEMBL508108 | — | — | 1 | 7.05 |
| CHEMBL507006 | — | — | 1 | 7.00 |
| CHEMBL507686 | — | — | 1 | 6.92 |
| CHEMBL507295 | — | — | 1 | 6.92 |
| CHEMBL448760 | — | — | 1 | 6.89 |
| CHEMBL509544 | — | — | 1 | 6.89 |
| CHEMBL446276 | — | — | 1 | 6.80 |
| CHEMBL499795 | — | — | 1 | 6.75 |
| CHEMBL506902 | — | — | 1 | 6.68 |
| CHEMBL449831 | — | — | 1 | 6.66 |
| CHEMBL478720 | — | — | 1 | 6.40 |
| CHEMBL455328 | — | — | 1 | 6.38 |
| CHEMBL500059 | — | — | 1 | 6.33 |
| CHEMBL117315 | — | — | 1 | 6.22 |
| CHEMBL475683 | — | — | 1 | 6.10 |
| CHEMBL463738 | — | — | 1 | 5.77 |
| CHEMBL447826 | — | — | 1 | 5.75 |
| CHEMBL455326 | — | — | 1 | 5.22 |
| CHEMBL503252 | — | — | 1 | 5.19 |
| CHEMBL452445 | — | — | 1 | 5.00 |
| CHEMBL447330 | — | — | 1 | 5.00 |
| CHEMBL502679 | — | — | 1 | - |
| CHEMBL510006 | — | — | 1 | - |
| CHEMBL450991 | — | — | 1 | - |
| CHEMBL499103 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL435191 | EDOTECARIN | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL505815 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL503051 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL474561 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL454734 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL508108 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL507006 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL507686 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL507295 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL448760 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL509544 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL446276 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL499795 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL506902 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL449831 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL478720 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL455328 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL500059 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL117315 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL475683 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL463738 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL447826 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL455326 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL503252 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL452445 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL447330 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL502679 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL510006 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL450991 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL499103 | — | EC50 | > | 10000.0 | nM | - |