Assay Detail
Functional
CHEMBL1640706
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-BR-3 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.11 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 8.70 |
| CHEMBL1630113 | — | — | 1 | 6.58 |
| CHEMBL1630117 | — | — | 1 | 6.57 |
| CHEMBL1630110 | — | — | 1 | 6.48 |
| CHEMBL1630109 | — | — | 1 | 6.46 |
| CHEMBL1630118 | — | — | 1 | 6.38 |
| CHEMBL1630107 | — | — | 1 | 6.29 |
| CHEMBL1630112 | — | — | 1 | 6.21 |
| CHEMBL1630108 | — | — | 1 | 5.96 |
| CHEMBL1630111 | — | — | 1 | 5.89 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 5.58 |
| CHEMBL1630116 | — | — | 1 | 5.36 |
| CHEMBL1630115 | — | — | 1 | 4.77 |
| CHEMBL1630114 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL554 | LAPATINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1630113 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1630117 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1630110 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL1630109 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1630118 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL1630107 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1630112 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1630108 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1630111 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1630116 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL1630115 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1630114 | — | IC50 | = | 50000.0 | nM | 4.30 |