Assay Detail
Binding
CHEMBL4821486
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Inhibition of HDAC in human HeLa nuclear extracts using Boc-Lys (acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorescence based assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Subcellular | Nucleus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.39 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4859992 | — | — | 1 | 7.70 |
| CHEMBL4874716 | — | — | 1 | 7.52 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.40 |
| CHEMBL4852441 | — | — | 1 | 7.40 |
| CHEMBL4861336 | — | — | 1 | 7.10 |
| CHEMBL4862510 | — | — | 1 | 7.00 |
| CHEMBL4796066 | — | — | 1 | 6.80 |
| CHEMBL4530950 | — | — | 1 | 6.54 |
| CHEMBL4877805 | — | — | 1 | 6.48 |
| CHEMBL4545246 | — | — | 1 | 6.46 |
| CHEMBL4877300 | — | — | 1 | 6.17 |
| CHEMBL4472834 | — | — | 1 | 6.08 |
| CHEMBL4874671 | — | — | 1 | 6.00 |
| CHEMBL4846564 | — | — | 1 | 5.79 |
| CHEMBL4872697 | — | — | 1 | 5.78 |
| CHEMBL4847771 | — | — | 1 | 5.77 |
| CHEMBL4858210 | — | — | 1 | 5.71 |
| CHEMBL4877023 | — | — | 1 | 5.67 |
| CHEMBL4473451 | — | — | 1 | 5.56 |
| CHEMBL4438566 | — | — | 1 | 4.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4859992 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4874716 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4852441 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4861336 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4862510 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4796066 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4530950 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4877805 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4545246 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4877300 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4472834 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4874671 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4846564 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL4872697 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL4847771 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL4858210 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL4877023 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL4473451 | — | IC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL4438566 | — | IC50 | = | 14960.0 | nM | 4.83 |