Assay Detail
Functional
CHEMBL1000708
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Cytotoxicity against multidrug resistant human KBV1 cells overexpressing MDR1 by MTT method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KB-V1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Cytotoxicity and TOP1-targeting activity of 8- and 9-amino derivatives of 5-butyl- and 5-(2-N,N-dimethylamino)ethyl-5H-dibenzo[c,h][1,6]naphthyridin-6-ones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.31 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL309355 | — | — | 1 | 8.40 |
| CHEMBL72772 | — | — | 1 | 7.60 |
| CHEMBL309352 | — | — | 1 | 6.89 |
| CHEMBL528538 | — | — | 1 | 6.72 |
| CHEMBL72223 | — | — | 1 | 6.55 |
| CHEMBL73950 | — | — | 1 | 6.52 |
| CHEMBL487129 | — | — | 1 | 6.39 |
| CHEMBL84 | TOPOTECAN | 4.0 | 1 | 6.36 |
| CHEMBL486928 | — | — | 1 | 6.26 |
| CHEMBL488371 | — | — | 1 | 6.22 |
| CHEMBL483808 | — | — | 1 | 6.07 |
| CHEMBL487130 | — | — | 1 | 5.70 |
| CHEMBL306476 | — | — | 1 | 5.60 |
| CHEMBL484993 | — | — | 1 | 5.60 |
| CHEMBL488370 | — | — | 1 | 5.58 |
| CHEMBL486929 | — | — | 1 | 5.50 |
| CHEMBL485170 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL309355 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL72772 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL309352 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL528538 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL72223 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL73950 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL487129 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL84 | TOPOTECAN | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL486928 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL488371 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL483808 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL487130 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL306476 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL484993 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL488370 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL486929 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL485170 | — | IC50 | = | 4500.0 | nM | 5.35 |