Assay Detail
Binding
CHEMBL840259
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Effective concentration against DNA topoisomerase I
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.40 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL307794 | — | — | 1 | 7.30 |
| CHEMBL837 | 7-ETHYL-10-HYDROXYCAMPTOTHECIN | 2.0 | 2 | 7.16 |
| CHEMBL184094 | — | — | 1 | 6.82 |
| CHEMBL364360 | — | — | 1 | 6.80 |
| CHEMBL181547 | — | — | 1 | 6.72 |
| CHEMBL184100 | — | — | 1 | 6.70 |
| CHEMBL364827 | — | — | 1 | 6.62 |
| CHEMBL183350 | — | — | 1 | 6.57 |
| CHEMBL65 | CAMPTOTHECIN | -1.0 | 1 | 6.46 |
| CHEMBL186541 | — | — | 1 | 6.35 |
| CHEMBL359567 | — | — | 1 | 6.00 |
| CHEMBL361594 | — | — | 1 | 5.98 |
| CHEMBL185306 | — | — | 1 | 5.94 |
| CHEMBL360812 | — | — | 1 | 5.86 |
| CHEMBL363752 | — | — | 1 | 5.71 |
| CHEMBL188121 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL307794 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL837 | 7-ETHYL-10-HYDROXYCAMPTOTHECIN | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL184094 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL364360 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL181547 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL184100 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL364827 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL183350 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL837 | 7-ETHYL-10-HYDROXYCAMPTOTHECIN | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL65 | CAMPTOTHECIN | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL186541 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL359567 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL361594 | — | EC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL185306 | — | EC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL360812 | — | EC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL363752 | — | EC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL188121 | — | EC50 | = | 4560.0 | nM | 5.34 |