Assay Detail
ADMET
CHEMBL4416954
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His-tagged human HDAC3 (1 to 428 residues)/N-terminal GST tagged human NCOR2 (395 to 489) expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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
Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.16 | 5.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448978 | — | — | 1 | 5.78 |
| CHEMBL4439302 | — | — | 1 | 5.54 |
| CHEMBL4469978 | — | — | 1 | 5.45 |
| CHEMBL4591933 | — | — | 1 | 5.30 |
| CHEMBL155579 | — | — | 1 | 4.74 |
| CHEMBL16300 | BENZOHYDROXAMATE | — | 1 | 4.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448978 | — | IC50 | = | 1671.0 | nM | 5.78 |
| CHEMBL4439302 | — | IC50 | = | 2896.0 | nM | 5.54 |
| CHEMBL4469978 | — | IC50 | = | 3563.0 | nM | 5.45 |
| CHEMBL4591933 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL155579 | — | IC50 | = | 18402.0 | nM | 4.74 |
| CHEMBL16300 | BENZOHYDROXAMATE | IC50 | = | 71572.0 | nM | 4.14 |