Assay Detail
Binding
CHEMBL4823343
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human C-terminal His-fusion tagged/N-terminal Strep2 tagged HDAC8 (1 to 377 residues) expressed in insect cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorimetry
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
Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.18 | 5.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 5.65 |
| CHEMBL4876405 | — | — | 1 | 5.42 |
| CHEMBL4875953 | — | — | 1 | 5.10 |
| CHEMBL4866536 | — | — | 1 | 5.01 |
| CHEMBL4850081 | — | — | 1 | 4.99 |
| CHEMBL4870868 | — | — | 1 | 4.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL4876405 | — | IC50 | = | 3790.0 | nM | 5.42 |
| CHEMBL4875953 | — | IC50 | = | 7950.0 | nM | 5.10 |
| CHEMBL4866536 | — | IC50 | = | 9780.0 | nM | 5.01 |
| CHEMBL4850081 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL4870868 | — | IC50 | = | 12400.0 | nM | 4.91 |