Assay Detail
Functional
CHEMBL926029
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Antiproliferative activity against BCRP overexpressing mitoxantrone-resistant human HT29 cells after 1 hr of drug exposure measured after 72 hrs
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.83 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL111767 | — | — | 1 | 7.38 |
| CHEMBL113051 | GIMATECAN | 2.0 | 1 | 7.16 |
| CHEMBL256714 | — | — | 1 | 6.46 |
| CHEMBL255713 | — | — | 1 | 6.25 |
| CHEMBL74190 | HOMOCAMPTOTHECIN | — | 1 | 5.07 |
| CHEMBL65 | CAMPTOTHECIN | -1.0 | 1 | 5.05 |
| CHEMBL837 | 7-ETHYL-10-HYDROXYCAMPTOTHECIN | 2.0 | 1 | 4.94 |
| CHEMBL84 | TOPOTECAN | 4.0 | 1 | 4.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL111767 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL113051 | GIMATECAN | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL256714 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL255713 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL74190 | HOMOCAMPTOTHECIN | IC50 | = | 8550.0 | nM | 5.07 |
| CHEMBL65 | CAMPTOTHECIN | IC50 | = | 8810.0 | nM | 5.05 |
| CHEMBL837 | 7-ETHYL-10-HYDROXYCAMPTOTHECIN | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL84 | TOPOTECAN | IC50 | = | 46290.0 | nM | 4.33 |