Assay Detail
Binding
CHEMBL4233455
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Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate pretreated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
9
Total Activities
9
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 anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.52 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4241141 | — | — | 1 | 8.41 |
| CHEMBL4240694 | — | — | 1 | 8.29 |
| CHEMBL4237410 | — | — | 1 | 8.09 |
| CHEMBL4251261 | — | — | 1 | 7.85 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.84 |
| CHEMBL4248226 | — | — | 1 | 7.18 |
| CHEMBL4248676 | — | — | 1 | 6.87 |
| CHEMBL4244419 | — | — | 1 | 6.65 |
| CHEMBL4244887 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4241141 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4240694 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4237410 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4251261 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL4248226 | — | IC50 | = | 66.2 | nM | 7.18 |
| CHEMBL4248676 | — | IC50 | = | 133.8 | nM | 6.87 |
| CHEMBL4244419 | — | IC50 | = | 224.3 | nM | 6.65 |
| CHEMBL4244887 | — | IC50 | = | 306.2 | nM | 6.51 |