Assay Detail
Binding
CHEMBL1640688
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Inhibition of HDAC in human HeLa cell nuclear extracts
18
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 5 — Multiple protein complex / RNA |
| 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 | 15 | 5.91 | 7.33 |
| Emax | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1630109 | — | — | 1 | 7.33 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.16 |
| CHEMBL1630118 | — | — | 2 | 6.37 |
| CHEMBL1630107 | — | — | 1 | 6.20 |
| CHEMBL1630117 | — | — | 2 | 5.08 |
| CHEMBL514671 | — | — | 1 | 4.96 |
| CHEMBL1630108 | — | — | 1 | 4.30 |
| CHEMBL1630110 | — | — | 1 | - |
| CHEMBL1630111 | — | — | 1 | - |
| CHEMBL1630112 | — | — | 2 | - |
| CHEMBL1630113 | — | — | 1 | - |
| CHEMBL1630114 | — | — | 1 | - |
| CHEMBL1630115 | — | — | 1 | - |
| CHEMBL1630116 | — | — | 1 | - |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1630109 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1630118 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1630107 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL1630117 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL514671 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1630108 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL1630111 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1630112 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1630113 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630114 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630115 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630116 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL554 | LAPATINIB | IC50 | > | 100000.0 | nM | - |
| CHEMBL1630112 | — | Emax | = | 20.0 | % | - |
| CHEMBL1630117 | — | Emax | = | 30.0 | % | - |
| CHEMBL1630110 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630118 | — | Emax | = | 65.0 | % | - |