Assay Detail
Binding
CHEMBL4685117
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Inhibition of recombinant human C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorimetry analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.92 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 8.16 |
| CHEMBL4790559 | — | — | 1 | 6.26 |
| CHEMBL4790152 | — | — | 1 | 5.97 |
| CHEMBL4789155 | — | — | 1 | 5.73 |
| CHEMBL4747757 | — | — | 1 | 5.50 |
| CHEMBL4798549 | — | — | 1 | 5.42 |
| CHEMBL4741850 | — | — | 1 | 5.16 |
| CHEMBL4740842 | — | — | 1 | 5.13 |
| CHEMBL4782478 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 6.96 | nM | 8.16 |
| CHEMBL4790559 | — | IC50 | = | 554.0 | nM | 6.26 |
| CHEMBL4790152 | — | IC50 | = | 1075.0 | nM | 5.97 |
| CHEMBL4789155 | — | IC50 | = | 1878.0 | nM | 5.73 |
| CHEMBL4747757 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL4798549 | — | IC50 | = | 3814.0 | nM | 5.42 |
| CHEMBL4741850 | — | IC50 | = | 6885.0 | nM | 5.16 |
| CHEMBL4740842 | — | IC50 | = | 7431.0 | nM | 5.13 |
| CHEMBL4782478 | — | IC50 | > | 10000.0 | nM | - |