Assay Detail
Binding
CHEMBL821422
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Inhibit supercoil relaxation property of topoisomerase I.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Camptothecin and minor-groove binder hybrid molecules: synthesis, inhibition of topoisomerase I, and anticancer cytotoxicity in vitro.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.39 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL65 | CAMPTOTHECIN | -1.0 | 1 | 6.16 |
| CHEMBL72627 | — | — | 1 | 5.95 |
| CHEMBL266468 | — | — | 1 | 5.71 |
| CHEMBL311855 | — | — | 1 | 5.62 |
| CHEMBL312306 | — | — | 1 | 5.62 |
| CHEMBL72828 | — | — | 1 | 5.58 |
| CHEMBL11252 | STALLIMYCIN | 2.0 | 1 | 5.57 |
| CHEMBL73002 | — | — | 1 | 5.41 |
| CHEMBL72353 | — | — | 1 | 5.37 |
| CHEMBL312690 | — | — | 1 | 5.34 |
| CHEMBL74459 | — | — | 1 | 5.32 |
| CHEMBL64874 | — | — | 1 | 5.32 |
| CHEMBL386919 | — | — | 1 | 4.92 |
| CHEMBL74406 | — | — | 1 | 4.78 |
| CHEMBL307767 | NETROPSIN | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL65 | CAMPTOTHECIN | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL72627 | — | IC50 | = | 1118.0 | nM | 5.95 |
| CHEMBL266468 | — | IC50 | = | 1973.0 | nM | 5.71 |
| CHEMBL311855 | — | IC50 | = | 2417.0 | nM | 5.62 |
| CHEMBL312306 | — | IC50 | = | 2382.0 | nM | 5.62 |
| CHEMBL72828 | — | IC50 | = | 2602.0 | nM | 5.58 |
| CHEMBL11252 | STALLIMYCIN | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL73002 | — | IC50 | = | 3882.0 | nM | 5.41 |
| CHEMBL72353 | — | IC50 | = | 4290.0 | nM | 5.37 |
| CHEMBL312690 | — | IC50 | = | 4597.0 | nM | 5.34 |
| CHEMBL74459 | — | IC50 | = | 4842.0 | nM | 5.32 |
| CHEMBL64874 | — | IC50 | = | 4818.0 | nM | 5.32 |
| CHEMBL386919 | — | IC50 | = | 11918.0 | nM | 4.92 |
| CHEMBL74406 | — | IC50 | = | 16618.0 | nM | 4.78 |
| CHEMBL307767 | NETROPSIN | IC50 | = | 62000.0 | nM | 4.21 |