Assay Detail
Binding
CHEMBL4346117
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human HDAC2 expressed in baculovirus expression system using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis
26
Total Activities
26
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 of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.21 | 7.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 1 | 7.88 |
| CHEMBL4444219 | — | — | 1 | 7.30 |
| CHEMBL4534191 | — | — | 1 | 7.17 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.05 |
| CHEMBL27759 | ENTINOSTAT | 3.0 | 1 | 6.97 |
| CHEMBL4531072 | — | — | 1 | 6.97 |
| CHEMBL4435691 | — | — | 1 | 6.76 |
| CHEMBL4474900 | — | — | 1 | 6.76 |
| CHEMBL4555545 | — | — | 1 | 6.55 |
| CHEMBL4583564 | — | — | 1 | 6.36 |
| CHEMBL4465293 | — | — | 1 | 6.32 |
| CHEMBL4558922 | — | — | 1 | 6.24 |
| CHEMBL4580907 | — | — | 1 | 5.89 |
| CHEMBL4515793 | — | — | 1 | 5.87 |
| CHEMBL4459612 | — | — | 1 | 5.49 |
| CHEMBL4457985 | — | — | 1 | 5.38 |
| CHEMBL4443074 | — | — | 1 | 5.31 |
| CHEMBL4465023 | — | — | 1 | 5.14 |
| CHEMBL4475018 | — | — | 1 | 5.09 |
| CHEMBL4448939 | — | — | 1 | 5.01 |
| CHEMBL4545275 | — | — | 1 | 4.89 |
| CHEMBL4457133 | — | — | 1 | - |
| CHEMBL4452554 | — | — | 1 | - |
| CHEMBL4526716 | — | — | 1 | - |
| CHEMBL4482900 | — | — | 1 | - |
| CHEMBL4449713 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL4444219 | — | IC50 | = | 49.5 | nM | 7.30 |
| CHEMBL4534191 | — | IC50 | = | 67.48 | nM | 7.17 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 89.23 | nM | 7.05 |
| CHEMBL27759 | ENTINOSTAT | IC50 | = | 108.2 | nM | 6.97 |
| CHEMBL4531072 | — | IC50 | = | 107.5 | nM | 6.97 |
| CHEMBL4435691 | — | IC50 | = | 174.6 | nM | 6.76 |
| CHEMBL4474900 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL4555545 | — | IC50 | = | 278.6 | nM | 6.55 |
| CHEMBL4583564 | — | IC50 | = | 441.3 | nM | 6.36 |
| CHEMBL4465293 | — | IC50 | = | 474.1 | nM | 6.32 |
| CHEMBL4558922 | — | IC50 | = | 579.3 | nM | 6.24 |
| CHEMBL4580907 | — | IC50 | = | 1298.0 | nM | 5.89 |
| CHEMBL4515793 | — | IC50 | = | 1366.0 | nM | 5.87 |
| CHEMBL4459612 | — | IC50 | = | 3222.0 | nM | 5.49 |
| CHEMBL4457985 | — | IC50 | = | 4214.0 | nM | 5.38 |
| CHEMBL4443074 | — | IC50 | = | 4942.0 | nM | 5.31 |
| CHEMBL4465023 | — | IC50 | = | 7316.0 | nM | 5.14 |
| CHEMBL4475018 | — | IC50 | = | 8071.0 | nM | 5.09 |
| CHEMBL4448939 | — | IC50 | = | 9835.0 | nM | 5.01 |
| CHEMBL4545275 | — | IC50 | = | 12930.0 | nM | 4.89 |
| CHEMBL4457133 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4452554 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4526716 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4482900 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4449713 | — | IC50 | > | 10000.0 | nM | - |