Assay Detail
Binding
CHEMBL4685844
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Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC 2A substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay
13
Total Activities
13
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
Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.23 | 6.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4757035 | — | — | 1 | 6.23 |
| CHEMBL4762873 | — | — | 1 | 6.19 |
| CHEMBL4757768 | — | — | 1 | 5.71 |
| CHEMBL4761847 | — | — | 1 | 5.51 |
| CHEMBL4753795 | — | — | 1 | 5.34 |
| CHEMBL4796066 | — | — | 1 | 5.04 |
| CHEMBL4750838 | — | — | 1 | 4.99 |
| CHEMBL4753828 | — | — | 1 | 4.77 |
| CHEMBL4751082 | — | — | 1 | 4.75 |
| CHEMBL4248676 | — | — | 1 | 4.50 |
| CHEMBL4752558 | — | — | 1 | 4.49 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
| CHEMBL4799871 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4757035 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4762873 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4757768 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL4761847 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4753795 | — | IC50 | = | 4570.0 | nM | 5.34 |
| CHEMBL4796066 | — | IC50 | = | 9130.0 | nM | 5.04 |
| CHEMBL4750838 | — | IC50 | = | 10290.0 | nM | 4.99 |
| CHEMBL4753828 | — | IC50 | = | 16840.0 | nM | 4.77 |
| CHEMBL4751082 | — | IC50 | = | 17880.0 | nM | 4.75 |
| CHEMBL4248676 | — | IC50 | = | 31530.0 | nM | 4.50 |
| CHEMBL4752558 | — | IC50 | = | 32670.0 | nM | 4.49 |
| CHEMBL98 | VORINOSTAT | IC50 | > | 40000.0 | nM | - |
| CHEMBL4799871 | — | IC50 | > | 40000.0 | nM | - |