Assay Detail
Functional
CHEMBL658281
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity using camptothecin-resistant variant of RPM18402 (CPT-K5) possessing functional, but mutant TOP-1
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RPMI 8402 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Diaza- and triazachrysenes: potent topoisomerase-targeting agents with exceptional antitumor activity against the human tumor xenograft, MDA-MB-435.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.79 | 6.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL452231 | TENIPOSIDE | 4.0 | 1 | 6.55 |
| CHEMBL71086 | — | — | 1 | 6.22 |
| CHEMBL70790 | — | — | 1 | 6.05 |
| CHEMBL331376 | — | — | 1 | 5.47 |
| CHEMBL113470 | — | — | 1 | 5.44 |
| CHEMBL113970 | — | — | 1 | 5.00 |
| CHEMBL321593 | — | — | 1 | - |
| CHEMBL326615 | — | — | 1 | - |
| CHEMBL84 | TOPOTECAN | 4.0 | 1 | - |
| CHEMBL113338 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL452231 | TENIPOSIDE | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL71086 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL70790 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL331376 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL113470 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL113970 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL321593 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL326615 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL84 | TOPOTECAN | IC50 | > | 10000.0 | nM | - |
| CHEMBL113338 | — | IC50 | > | 10000.0 | nM | - |