Assay Detail
Binding
CHEMBL1640689
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HDAC assessed as histone H3K'9+14 acetylation levels by cell based histone H3 hyperacetylation assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| EC50 | 15 | 5.40 | 5.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL514671 | — | — | 1 | 5.63 |
| CHEMBL1630107 | — | — | 1 | 5.44 |
| CHEMBL1630109 | — | — | 1 | 5.33 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 5.18 |
| CHEMBL1630108 | — | — | 1 | - |
| CHEMBL1630110 | — | — | 1 | - |
| CHEMBL1630111 | — | — | 1 | - |
| CHEMBL1630112 | — | — | 1 | - |
| CHEMBL1630115 | — | — | 1 | - |
| CHEMBL1630116 | — | — | 1 | - |
| CHEMBL1630117 | — | — | 1 | - |
| CHEMBL1630118 | — | — | 1 | - |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | - |
| CHEMBL1630114 | — | — | 1 | - |
| CHEMBL1630113 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL514671 | — | EC50 | = | 2350.0 | nM | 5.63 |
| CHEMBL1630107 | — | EC50 | = | 3650.0 | nM | 5.44 |
| CHEMBL1630109 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL98 | VORINOSTAT | EC50 | = | 6670.0 | nM | 5.18 |
| CHEMBL1630108 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL1630110 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1630111 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL1630112 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL1630115 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL1630116 | — | EC50 | - | — | - | |
| CHEMBL1630117 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL1630118 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL554 | LAPATINIB | EC50 | > | 30000.0 | nM | - |
| CHEMBL1630114 | — | EC50 | >= | 20000.0 | nM | - |
| CHEMBL1630113 | — | EC50 | - | — | - |