Assay Detail
Binding
CHEMBL4193699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full-length human C-terminal FLAG-His-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using Boc-L-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 35 mins by fluorescence assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.20 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4213297 | — | — | 1 | 7.01 |
| CHEMBL4208901 | — | — | 1 | 6.47 |
| CHEMBL4209843 | — | — | 1 | 6.11 |
| CHEMBL4212751 | — | — | 1 | 5.96 |
| CHEMBL4217705 | — | — | 1 | 5.75 |
| CHEMBL4206987 | — | — | 1 | 5.62 |
| CHEMBL2170177 | — | — | 1 | 5.42 |
| CHEMBL4210933 | — | — | 1 | 5.36 |
| CHEMBL4208780 | — | — | 1 | 5.14 |
| CHEMBL4206571 | — | — | 1 | 4.89 |
| CHEMBL4216233 | — | — | 1 | 4.85 |
| CHEMBL4214404 | — | — | 1 | 4.75 |
| CHEMBL4211873 | — | — | 1 | 4.75 |
| CHEMBL4218825 | — | — | 1 | 4.62 |
| CHEMBL4218293 | — | — | 1 | 4.57 |
| CHEMBL4208365 | — | — | 1 | 4.48 |
| CHEMBL4213891 | — | — | 1 | 4.43 |
| CHEMBL4078522 | — | — | 1 | 4.30 |
| CHEMBL4204967 | — | — | 1 | 4.24 |
| CHEMBL4206055 | — | — | 1 | - |
| CHEMBL4209492 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4213297 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4208901 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4209843 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4212751 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4217705 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4206987 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2170177 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4210933 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4208780 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4206571 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4216233 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4214404 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4211873 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4218825 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4218293 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4208365 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4213891 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL4078522 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL4204967 | — | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL4206055 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4209492 | — | IC50 | > | 100000.0 | nM | - |