Assay Detail
Binding
CHEMBL4394938
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant His-tagged HDAC2 (1 to 582 residues) expressed in baculovirus infected insect cells using FLUOR DE LYS Green as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.35 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4474354 | — | — | 1 | 6.80 |
| CHEMBL4573943 | — | — | 1 | 6.75 |
| CHEMBL4087968 | — | — | 1 | 6.51 |
| CHEMBL4589605 | — | — | 1 | 6.28 |
| CHEMBL4538745 | — | — | 1 | 6.21 |
| CHEMBL27759 | ENTINOSTAT | 3.0 | 1 | 6.17 |
| CHEMBL235191 | TACEDINALINE | 3.0 | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4474354 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4573943 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4087968 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4589605 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4538745 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL27759 | ENTINOSTAT | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL235191 | TACEDINALINE | IC50 | = | 1920.0 | nM | 5.72 |