Assay Detail
Binding
CHEMBL1640692
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Inhibition of Flag tagged human recombinant HDAC3 expressed in Sf21 cells coexpressing SMRT DAD domain
16
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| 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 | 6.45 | 7.43 |
| Emax | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.43 |
| CHEMBL1630109 | — | — | 1 | 7.18 |
| CHEMBL1630118 | — | — | 2 | 6.25 |
| CHEMBL514671 | — | — | 1 | 6.21 |
| CHEMBL1630107 | — | — | 1 | 5.20 |
| CHEMBL1630108 | — | — | 1 | - |
| CHEMBL1630110 | — | — | 1 | - |
| CHEMBL1630111 | — | — | 1 | - |
| CHEMBL1630112 | — | — | 1 | - |
| CHEMBL1630113 | — | — | 1 | - |
| CHEMBL1630114 | — | — | 1 | - |
| CHEMBL1630115 | — | — | 1 | - |
| CHEMBL1630116 | — | — | 1 | - |
| CHEMBL1630117 | — | — | 1 | - |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1630109 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1630118 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL514671 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1630107 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1630108 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630110 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630111 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630112 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630113 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630114 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630115 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630116 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL1630117 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL554 | LAPATINIB | IC50 | > | 10000.0 | nM | - |
| CHEMBL1630118 | — | Emax | = | 75.0 | % | - |