Assay Detail
Binding
CHEMBL5351712
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Inhibition of human HDAC8 expressed in baculovirus expression system in Sf9 cells using RHKAcKAc (379 to 382 residues) fluorogenic peptide as substrate and measured after 2 hrs by fluorescence based analysis
23
Total Activities
23
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 | 23 | 6.25 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5436391 | — | — | 1 | 6.89 |
| CHEMBL5438457 | — | — | 1 | 6.86 |
| CHEMBL5403206 | — | — | 1 | 6.81 |
| CHEMBL5404245 | — | — | 1 | 6.65 |
| CHEMBL5412013 | — | — | 1 | 6.59 |
| CHEMBL2425952 | — | — | 1 | 6.55 |
| CHEMBL5413612 | — | — | 1 | 6.55 |
| CHEMBL5401169 | — | — | 1 | 6.52 |
| CHEMBL4550214 | — | — | 1 | 6.51 |
| CHEMBL5423557 | — | — | 1 | 6.49 |
| CHEMBL5394143 | — | — | 1 | 6.43 |
| CHEMBL5396951 | — | — | 1 | 6.40 |
| CHEMBL5402184 | — | — | 1 | 6.34 |
| CHEMBL4554270 | — | — | 1 | 6.28 |
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 6.23 |
| CHEMBL5424549 | — | — | 1 | 6.01 |
| CHEMBL4513424 | — | — | 1 | 5.84 |
| CHEMBL2425955 | — | — | 1 | 5.81 |
| CHEMBL5437069 | — | — | 1 | 5.79 |
| CHEMBL5404427 | — | — | 1 | 5.43 |
| CHEMBL5424996 | — | — | 1 | 5.43 |
| CHEMBL5427585 | — | — | 1 | 4.98 |
| CHEMBL4464975 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5436391 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5438457 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5403206 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL5404245 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL5412013 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL2425952 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL5413612 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL5401169 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL4550214 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL5423557 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL5394143 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL5396951 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5402184 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL4554270 | — | IC50 | = | 525.0 | nM | 6.28 |
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 589.0 | nM | 6.23 |
| CHEMBL5424549 | — | IC50 | = | 966.0 | nM | 6.01 |
| CHEMBL4513424 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL2425955 | — | IC50 | = | 1555.0 | nM | 5.81 |
| CHEMBL5437069 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL5404427 | — | IC50 | = | 3730.0 | nM | 5.43 |
| CHEMBL5424996 | — | IC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL5427585 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL4464975 | — | IC50 | - | — | - |