Assay Detail
Binding
CHEMBL3762511
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Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay
18
Total Activities
18
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
Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.11 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3759562 | — | — | 1 | 7.75 |
| CHEMBL3760013 | — | — | 1 | 7.66 |
| CHEMBL3758882 | — | — | 1 | 7.58 |
| CHEMBL3758261 | — | — | 1 | 7.57 |
| CHEMBL3759791 | — | — | 1 | 7.52 |
| CHEMBL3759322 | — | — | 1 | 7.48 |
| CHEMBL3760115 | — | — | 1 | 7.25 |
| CHEMBL325676 | — | — | 1 | 7.13 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.09 |
| CHEMBL3759998 | — | — | 1 | 7.08 |
| CHEMBL3759941 | — | — | 1 | 7.04 |
| CHEMBL3758334 | — | — | 1 | 6.97 |
| CHEMBL3760046 | — | — | 1 | 6.78 |
| CHEMBL3759836 | — | — | 1 | 6.63 |
| CHEMBL3758451 | — | — | 1 | 6.62 |
| CHEMBL3758595 | — | — | 1 | 6.61 |
| CHEMBL3758444 | — | — | 1 | 6.12 |
| CHEMBL3758409 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3759562 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3760013 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3758882 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3758261 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3759791 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3759322 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3760115 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL325676 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3759998 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3759941 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3758334 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL3760046 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL3759836 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL3758451 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL3758595 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL3758444 | — | IC50 | = | 758.0 | nM | 6.12 |
| CHEMBL3758409 | — | IC50 | - | — | - |