Assay Detail
Functional
CHEMBL3267477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
22
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
A rational design strategy of the novel topoisomerase II inhibitors for the synthesis of the 4-O-(2-pyrazinecarboxylic)-4'-demethylepipodophyllotoxin with antitumor activity by diminishing the relaxation reaction of topoisomerase II-DNA decatenation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.21 | 6.22 |
| Activity | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3264611 | — | — | 2 | 6.22 |
| CHEMBL3264614 | — | — | 2 | 6.22 |
| CHEMBL3264613 | — | — | 2 | 6.19 |
| CHEMBL3264618 | — | — | 2 | 5.50 |
| CHEMBL3264612 | — | — | 2 | 5.02 |
| CHEMBL3264616 | — | — | 2 | 4.96 |
| CHEMBL31929 | 4'-DEMETHYLEPIPODOPHYLLOTOXIN | — | 2 | 4.80 |
| CHEMBL3264617 | — | — | 2 | 4.79 |
| CHEMBL3264615 | — | — | 2 | 4.69 |
| CHEMBL3264619 | — | — | 2 | 4.65 |
| CHEMBL44657 | ETOPOSIDE | 4.0 | 2 | 4.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3264611 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3264614 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3264613 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL3264618 | — | IC50 | = | 3180.0 | nM | 5.50 |
| CHEMBL3264612 | — | IC50 | = | 9560.0 | nM | 5.02 |
| CHEMBL3264616 | — | IC50 | = | 10840.0 | nM | 4.96 |
| CHEMBL31929 | 4'-DEMETHYLEPIPODOPHYLLOTOXIN | IC50 | = | 15960.0 | nM | 4.80 |
| CHEMBL3264617 | — | IC50 | = | 16050.0 | nM | 4.79 |
| CHEMBL3264615 | — | IC50 | = | 20530.0 | nM | 4.69 |
| CHEMBL3264619 | — | IC50 | = | 22270.0 | nM | 4.65 |
| CHEMBL44657 | ETOPOSIDE | IC50 | = | 59380.0 | nM | 4.23 |
| CHEMBL3264611 | — | Activity | - | — | - | |
| CHEMBL3264612 | — | Activity | - | — | - | |
| CHEMBL3264613 | — | Activity | - | — | - | |
| CHEMBL3264614 | — | Activity | - | — | - | |
| CHEMBL3264615 | — | Activity | - | — | - | |
| CHEMBL3264616 | — | Activity | - | — | - | |
| CHEMBL3264617 | — | Activity | - | — | - | |
| CHEMBL3264618 | — | Activity | - | — | - | |
| CHEMBL3264619 | — | Activity | - | — | - | |
| CHEMBL31929 | 4'-DEMETHYLEPIPODOPHYLLOTOXIN | Activity | - | — | - | |
| CHEMBL44657 | ETOPOSIDE | Activity | - | — | - |