Assay Detail
Binding
CHEMBL3829033
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence 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
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.55 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3622533 | FIMEPINOSTAT | 2.0 | 1 | 8.74 |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 1 | 8.64 |
| CHEMBL3828518 | — | — | 1 | 8.59 |
| CHEMBL3827517 | — | — | 1 | 8.57 |
| CHEMBL3827894 | — | — | 1 | 8.48 |
| CHEMBL3827814 | — | — | 1 | 8.47 |
| CHEMBL3827281 | — | — | 1 | 8.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3622533 | FIMEPINOSTAT | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 2.27 | nM | 8.64 |
| CHEMBL3828518 | — | IC50 | = | 2.55 | nM | 8.59 |
| CHEMBL3827517 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3827894 | — | IC50 | = | 3.29 | nM | 8.48 |
| CHEMBL3827814 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3827281 | — | IC50 | = | 4.65 | nM | 8.33 |