Assay Detail
Binding
CHEMBL4686047
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length C-terminal FLAG-His tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and evaluation of N-phenyl-4-(2-phenylsulfonamido)-benzamides as microtubule-targeting agents in drug-resistant cancer cells, displaying HDAC inhibitory response.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.86 | 6.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27759 | ENTINOSTAT | 3.0 | 1 | 6.27 |
| CHEMBL4749443 | — | — | 1 | 5.97 |
| CHEMBL4788251 | — | — | 1 | 5.92 |
| CHEMBL4777009 | — | — | 1 | 5.26 |
| CHEMBL4757836 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27759 | ENTINOSTAT | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4749443 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL4788251 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL4777009 | — | IC50 | = | 5450.0 | nM | 5.26 |
| CHEMBL4757836 | — | IC50 | > | 10000.0 | nM | - |