Assay Detail
Binding
CHEMBL5351711
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Inhibition of human HDAC6 expressed in baculovirus expression system in Sf9 cells using RHKKAc (379 to 382 residues) fluorogenic peptide as substrate and measured after 2 hrs by fluorescence based analysis
25
Total Activities
25
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
Discovery of HDAC6, HDAC8, and 6/8 Inhibitors and Development of Cell-Based Drug Screening Models for the Treatment of TGF-β-Induced Idiopathic Pulmonary Fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.21 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 9.00 |
| CHEMBL5403206 | — | — | 1 | 8.80 |
| CHEMBL4550214 | — | — | 1 | 8.40 |
| CHEMBL5414629 | — | — | 1 | 8.28 |
| CHEMBL5404245 | — | — | 1 | 8.22 |
| CHEMBL5396951 | — | — | 1 | 8.22 |
| CHEMBL5438457 | — | — | 1 | 8.00 |
| CHEMBL4554270 | — | — | 1 | 7.96 |
| CHEMBL5413612 | — | — | 1 | 7.89 |
| CHEMBL5394143 | — | — | 1 | 7.75 |
| CHEMBL5423557 | — | — | 1 | 7.55 |
| CHEMBL4464975 | — | — | 1 | 7.46 |
| CHEMBL5409813 | — | — | 1 | 7.33 |
| CHEMBL5401169 | — | — | 1 | 7.24 |
| CHEMBL2425955 | — | — | 1 | 7.21 |
| CHEMBL2425952 | — | — | 1 | 7.10 |
| CHEMBL5412013 | — | — | 1 | 6.97 |
| CHEMBL5404427 | — | — | 1 | 6.78 |
| CHEMBL5424996 | — | — | 1 | 6.54 |
| CHEMBL5437069 | — | — | 1 | 6.50 |
| CHEMBL4513424 | — | — | 1 | 6.20 |
| CHEMBL5402184 | — | — | 1 | 6.10 |
| CHEMBL5424549 | — | — | 1 | 5.22 |
| CHEMBL5436391 | — | — | 1 | 4.87 |
| CHEMBL5427585 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5403206 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4550214 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5414629 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5404245 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5396951 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5438457 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4554270 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5413612 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5394143 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5423557 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4464975 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5409813 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5401169 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL2425955 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2425952 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5412013 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL5404427 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL5424996 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL5437069 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL4513424 | — | IC50 | = | 636.0 | nM | 6.20 |
| CHEMBL5402184 | — | IC50 | = | 798.0 | nM | 6.10 |
| CHEMBL5424549 | — | IC50 | = | 5950.0 | nM | 5.22 |
| CHEMBL5436391 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL5427585 | — | IC50 | = | 22000.0 | nM | 4.66 |