Assay Detail
Binding
CHEMBL4707191
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay
7
Total Activities
7
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
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.49 | 7.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3622533 | FIMEPINOSTAT | 2.0 | 1 | 7.27 |
| CHEMBL4785064 | — | — | 1 | 6.74 |
| CHEMBL4744689 | — | — | 1 | 6.57 |
| CHEMBL4749655 | — | — | 1 | 6.50 |
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 6.31 |
| CHEMBL1851943 | PRACINOSTAT | 3.0 | 1 | 5.55 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3622533 | FIMEPINOSTAT | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4785064 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL4744689 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4749655 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL1851943 | PRACINOSTAT | IC50 | = | 2835.0 | nM | 5.55 |
| CHEMBL98 | VORINOSTAT | IC50 | - | — | - |