Assay Detail
Binding
CHEMBL4190002
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Inhibition of ALDH1A1 in human SKOV3TR cells assessed as potentiation of 100 nM paclitaxel-mediated cytotoxicity after 4 days by CellTiter-Glo assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 5.42 | 5.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4213848 | — | — | 1 | 5.71 |
| CHEMBL4212457 | — | — | 1 | 5.65 |
| CHEMBL4206892 | — | — | 1 | 5.57 |
| CHEMBL3416562 | — | — | 1 | 5.52 |
| CHEMBL4215649 | — | — | 1 | 5.11 |
| CHEMBL4206272 | — | — | 1 | 4.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4213848 | — | EC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL4212457 | — | EC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL4206892 | — | EC50 | = | 2720.0 | nM | 5.57 |
| CHEMBL3416562 | — | EC50 | = | 3040.0 | nM | 5.52 |
| CHEMBL4215649 | — | EC50 | = | 7790.0 | nM | 5.11 |
| CHEMBL4206272 | — | EC50 | = | 11200.0 | nM | 4.95 |