Assay Detail
Binding
CHEMBL4685846
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Inhibition of recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) expressed in baculovirus infected Sf9 insect 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 | 5.38 | 6.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4761847 | — | — | 1 | 6.37 |
| CHEMBL4757035 | — | — | 1 | 6.16 |
| CHEMBL4762873 | — | — | 1 | 6.07 |
| CHEMBL4757768 | — | — | 1 | 5.78 |
| CHEMBL4248676 | — | — | 1 | 5.59 |
| CHEMBL4752558 | — | — | 1 | 5.47 |
| CHEMBL4753795 | — | — | 1 | 5.37 |
| CHEMBL4796066 | — | — | 1 | 5.14 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 4.98 |
| CHEMBL4750838 | — | — | 1 | 4.82 |
| CHEMBL4751082 | — | — | 1 | 4.80 |
| CHEMBL4799871 | — | — | 1 | 4.76 |
| CHEMBL4753828 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4761847 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4757035 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4762873 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4757768 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL4248676 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL4752558 | — | IC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL4753795 | — | IC50 | = | 4230.0 | nM | 5.37 |
| CHEMBL4796066 | — | IC50 | = | 7190.0 | nM | 5.14 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 10510.0 | nM | 4.98 |
| CHEMBL4750838 | — | IC50 | = | 15180.0 | nM | 4.82 |
| CHEMBL4751082 | — | IC50 | = | 15830.0 | nM | 4.80 |
| CHEMBL4799871 | — | IC50 | = | 17540.0 | nM | 4.76 |
| CHEMBL4753828 | — | IC50 | = | 20760.0 | nM | 4.68 |