Assay Detail
Binding
CHEMBL4707186
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human C-terminal His-tagged HDAC3 (1 to 428 end residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 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 | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) (CHEMBL2111363) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 8.33 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744689 | — | — | 1 | 9.18 |
| CHEMBL4749655 | — | — | 1 | 8.96 |
| CHEMBL4785064 | — | — | 1 | 8.70 |
| CHEMBL3622533 | FIMEPINOSTAT | 2.0 | 1 | 8.49 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.47 |
| CHEMBL1851943 | PRACINOSTAT | 3.0 | 1 | 7.16 |
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744689 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL4749655 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4785064 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3622533 | FIMEPINOSTAT | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1851943 | PRACINOSTAT | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL99 | TRICHOSTATIN | IC50 | - | — | - |