Assay Detail
Binding
CHEMBL3801294
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human HDAC3/NCOR1 complex expressed in insect cells assessed as residual enzyme activity preincubated for 1 hr followed by addition of fluorogenic Ac-LGK-ac-AMC as substrate for 30 mins by fluorescence analysis
4
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
A potent trifluoromethyl ketone histone deacetylase inhibitor exhibits class-dependent mechanism of action
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.41 | 9.27 |
| IC50 | 1 | 8.15 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 9.27 |
| CHEMBL113537 | — | — | 2 | 8.15 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL113537 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL98 | VORINOSTAT | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL113537 | — | Ki | = | 11.0 | nM | 7.96 |