Assay Detail
Binding
CHEMBL951649
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Inhibition of human 1 unit topoisomerase 2alpha catalytic activity assessed as relaxation of 198 ng supercoiled pBR322 DNA by agarose gel electrophoresis
10
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Screening of triterpenoids isolated from Phyllanthus flexuosus for DNA topoisomerase inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.57 | 4.98 |
| Activity | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289191 | LUPEOL | — | 2 | 4.98 |
| CHEMBL491188 | — | — | 2 | 4.76 |
| CHEMBL23236 | BETULIN | — | 2 | 4.41 |
| CHEMBL489552 | — | — | 2 | 4.41 |
| CHEMBL44657 | ETOPOSIDE | 4.0 | 1 | 4.30 |
| CHEMBL489551 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289191 | LUPEOL | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL491188 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL23236 | BETULIN | IC50 | = | 38600.0 | nM | 4.41 |
| CHEMBL489552 | — | IC50 | = | 38700.0 | nM | 4.41 |
| CHEMBL44657 | ETOPOSIDE | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL489551 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL491188 | — | Activity | - | — | - | |
| CHEMBL489552 | — | Activity | - | — | - | |
| CHEMBL289191 | LUPEOL | Activity | - | — | - | |
| CHEMBL23236 | BETULIN | Activity | - | — | - |