Assay Detail
Binding
CHEMBL4606153
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Inhibition of human recombinant HDAC8 pre-incubated for 30 mins before Ac-Leu- Gly-Lys(Ac)-AMC substrate addition and measured after 90 mins by fluorescence based assay
7
Total Activities
7
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
Achiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.17 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4640356 | — | — | 1 | 7.39 |
| CHEMBL4642874 | — | — | 1 | 7.36 |
| CHEMBL4634521 | — | — | 1 | 7.23 |
| CHEMBL4639966 | — | — | 1 | 7.16 |
| CHEMBL191091 | — | — | 1 | 7.06 |
| CHEMBL4636734 | — | — | 1 | 7.05 |
| CHEMBL4640415 | — | — | 1 | 6.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4640356 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4642874 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4634521 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4639966 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL191091 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4636734 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4640415 | — | IC50 | = | 118.0 | nM | 6.93 |