Assay Detail
Binding
CHEMBL5738227
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Histone Deacetylase Enzymatic Activity: The following non-trypsin coupled in-vitro HDAC enzymatic endpoint assay was used to assay the compounds of the invention. Below is a standardized protocol for running HDAC selectivity panel on Caliper LabChip EZ-Reader Instrument.
63
Total Activities
19
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Inhibitors of histone deacetylase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.65 | 8.40 |
| kon | 21 | - | - |
| k_off | 21 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6025816 | — | — | 3 | 8.40 |
| CHEMBL272980 | MOCETINOSTAT | 2.0 | 3 | 8.22 |
| CHEMBL3621988 | TUCIDINOSTAT | 3.0 | 3 | 8.05 |
| CHEMBL5845280 | — | — | 3 | 7.92 |
| CHEMBL27759 | ENTINOSTAT | 3.0 | 3 | 7.85 |
| CHEMBL235191 | TACEDINALINE | 3.0 | 6 | 7.41 |
| CHEMBL5872475 | — | — | 3 | 7.05 |
| CHEMBL5741150 | — | — | 3 | 6.92 |
| CHEMBL6058785 | — | — | 3 | 6.82 |
| CHEMBL4293858 | — | — | 6 | 5.90 |
| CHEMBL6045068 | — | — | 3 | 5.86 |
| CHEMBL5977797 | — | — | 3 | 5.76 |
| CHEMBL5779528 | — | — | 3 | 5.67 |
| CHEMBL5897350 | — | — | 3 | 5.66 |
| CHEMBL5831128 | — | — | 3 | 5.34 |
| CHEMBL5901312 | — | — | 3 | 5.10 |
| CHEMBL5880649 | — | — | 3 | 5.08 |
| CHEMBL6042323 | — | — | 3 | - |
| CHEMBL5982162 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6025816 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL272980 | MOCETINOSTAT | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3621988 | TUCIDINOSTAT | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5845280 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL27759 | ENTINOSTAT | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL235191 | TACEDINALINE | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL235191 | TACEDINALINE | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5872475 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5741150 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL6058785 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4293858 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4293858 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL6045068 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL5977797 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL5779528 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL5897350 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL5831128 | — | IC50 | = | 4560.0 | nM | 5.34 |
| CHEMBL5901312 | — | IC50 | = | 7950.0 | nM | 5.10 |
| CHEMBL5880649 | — | IC50 | = | 8260.0 | nM | 5.08 |
| CHEMBL6045068 | — | k_off | = | - | s-1 | - |
| CHEMBL6045068 | — | kon | = | - | — | - |
| CHEMBL6058785 | — | k_off | = | - | s-1 | - |
| CHEMBL6058785 | — | kon | = | - | — | - |
| CHEMBL5779528 | — | k_off | = | - | s-1 | - |
| CHEMBL5779528 | — | kon | = | - | — | - |
| CHEMBL5897350 | — | k_off | = | - | s-1 | - |
| CHEMBL5897350 | — | kon | = | - | — | - |
| CHEMBL4293858 | — | k_off | = | - | s-1 | - |
| CHEMBL4293858 | — | kon | = | - | — | - |
| CHEMBL235191 | TACEDINALINE | k_off | = | - | s-1 | - |
| CHEMBL235191 | TACEDINALINE | kon | = | - | — | - |
| CHEMBL5901312 | — | kon | = | - | — | - |
| CHEMBL3621988 | TUCIDINOSTAT | k_off | = | - | s-1 | - |
| CHEMBL3621988 | TUCIDINOSTAT | kon | = | - | — | - |
| CHEMBL6025816 | — | k_off | = | - | s-1 | - |
| CHEMBL6025816 | — | kon | = | - | — | - |
| CHEMBL5845280 | — | k_off | = | - | s-1 | - |
| CHEMBL5845280 | — | kon | = | - | — | - |
| CHEMBL272980 | MOCETINOSTAT | k_off | = | - | s-1 | - |
| CHEMBL272980 | MOCETINOSTAT | kon | = | - | — | - |
| CHEMBL5741150 | — | k_off | = | - | s-1 | - |
| CHEMBL5741150 | — | kon | = | - | — | - |
| CHEMBL27759 | ENTINOSTAT | k_off | = | - | s-1 | - |
| CHEMBL27759 | ENTINOSTAT | kon | = | - | — | - |
| CHEMBL5977797 | — | kon | = | - | — | - |
| CHEMBL4293858 | — | k_off | = | - | s-1 | - |
| CHEMBL235191 | TACEDINALINE | kon | = | - | — | - |
| CHEMBL4293858 | — | kon | = | - | — | - |
| CHEMBL5982162 | — | k_off | = | - | s-1 | - |
| CHEMBL235191 | TACEDINALINE | k_off | = | - | s-1 | - |