Assay Detail
Binding
CHEMBL3829049
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Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A2780 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
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 |
|---|---|---|---|
| EC50 | 8 | 6.84 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3828518 | — | — | 1 | 7.01 |
| CHEMBL3827814 | — | — | 1 | 6.95 |
| CHEMBL3827281 | — | — | 1 | 6.93 |
| CHEMBL3827894 | — | — | 1 | 6.91 |
| CHEMBL3622533 | FIMEPINOSTAT | 2.0 | 1 | 6.90 |
| CHEMBL3827517 | — | — | 1 | 6.85 |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 1 | 6.77 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3828518 | — | EC50 | = | 98.58 | nM | 7.01 |
| CHEMBL3827814 | — | EC50 | = | 112.96 | nM | 6.95 |
| CHEMBL3827281 | — | EC50 | = | 117.65 | nM | 6.93 |
| CHEMBL3827894 | — | EC50 | = | 123.2 | nM | 6.91 |
| CHEMBL3622533 | FIMEPINOSTAT | EC50 | = | 126.25 | nM | 6.90 |
| CHEMBL3827517 | — | EC50 | = | 142.01 | nM | 6.85 |
| CHEMBL483254 | PANOBINOSTAT | EC50 | = | 169.5 | nM | 6.77 |
| CHEMBL98 | VORINOSTAT | EC50 | = | 377.48 | nM | 6.42 |