Assay Detail
Binding
CHEMBL814847
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Average concentration to cause 50% inhibition of topo 1 using the cleavable complex assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.82 | 5.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL837 | 7-ETHYL-10-HYDROXYCAMPTOTHECIN | 2.0 | 1 | 5.40 |
| CHEMBL289665 | — | — | 1 | 5.30 |
| CHEMBL445883 | — | — | 1 | 4.92 |
| CHEMBL296862 | — | — | 1 | 4.80 |
| CHEMBL84 | TOPOTECAN | 4.0 | 1 | 4.70 |
| CHEMBL297811 | — | — | 1 | 4.68 |
| CHEMBL65 | CAMPTOTHECIN | -1.0 | 1 | 4.40 |
| CHEMBL44044 | — | — | 1 | 4.39 |
| CHEMBL288053 | — | — | 1 | - |
| CHEMBL41652 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL837 | 7-ETHYL-10-HYDROXYCAMPTOTHECIN | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL289665 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL445883 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL296862 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL84 | TOPOTECAN | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL297811 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL65 | CAMPTOTHECIN | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL44044 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL288053 | — | IC50 | = | 1600000.0 | nM | - |
| CHEMBL41652 | — | IC50 | = | 133000.0 | nM | - |