Assay Detail
Binding
CHEMBL5610305
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Inhibition of purified recombinant human HDAC6 assessed as inhibition constant using residues 379-382 (RHKK(Ac)AMC) fluorogenic substrate p53 fluorogenic peptide as substrate measured after 90 mins by fluorescence assay
15
Total Activities
15
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
Biological and structural investigation of tetrahydro-β-carboline-based selective HDAC6 inhibitors with improved stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 9.12 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5613232 | — | — | 1 | 9.51 |
| CHEMBL5613463 | — | — | 1 | 9.39 |
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 9.39 |
| CHEMBL5612869 | — | — | 1 | 9.36 |
| CHEMBL5614084 | — | — | 1 | 9.36 |
| CHEMBL4087616 | — | — | 1 | 9.15 |
| CHEMBL5613331 | — | — | 1 | 9.11 |
| CHEMBL5613501 | — | — | 1 | 8.97 |
| CHEMBL5613395 | — | — | 1 | 8.97 |
| CHEMBL5612190 | — | — | 1 | 8.91 |
| CHEMBL5612762 | — | — | 1 | 8.90 |
| CHEMBL5613532 | — | — | 1 | 8.79 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 8.71 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
| CHEMBL2105763 | QUISINOSTAT | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5613232 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL5613463 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL99 | TRICHOSTATIN | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL5612869 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL5614084 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL4087616 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL5613331 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL5613501 | — | Ki | = | 1.08 | nM | 8.97 |
| CHEMBL5613395 | — | Ki | = | 1.08 | nM | 8.97 |
| CHEMBL5612190 | — | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL5612762 | — | Ki | = | 1.25 | nM | 8.90 |
| CHEMBL5613532 | — | Ki | = | 1.64 | nM | 8.79 |
| CHEMBL2018302 | TUBASTATIN A | Ki | = | 1.97 | nM | 8.71 |
| CHEMBL98 | VORINOSTAT | Ki | - | — | - | |
| CHEMBL2105763 | QUISINOSTAT | Ki | - | — | - |