Assay Detail
Binding
CHEMBL3830868
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Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay
14
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.71 | 9.00 |
| Ki | 3 | 6.92 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 1 | 9.00 |
| CHEMBL3828396 | — | — | 2 | 7.54 |
| CHEMBL3827993 | — | — | 1 | 7.35 |
| CHEMBL3827363 | — | — | 1 | 7.14 |
| CHEMBL3827262 | — | — | 1 | 6.91 |
| CHEMBL3827611 | — | — | 2 | 6.75 |
| CHEMBL3827766 | — | — | 1 | 6.33 |
| CHEMBL3827412 | — | — | 1 | 5.91 |
| CHEMBL3828496 | — | — | 1 | 5.84 |
| CHEMBL3827055 | — | — | 1 | 5.84 |
| CHEMBL3828015 | — | — | 1 | 5.25 |
| CHEMBL235842 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3828396 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3827993 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3827363 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3828396 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL3827262 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL3827611 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL3827611 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL3827766 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL3827412 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL3828496 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL3827055 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL3828015 | — | IC50 | = | 5590.0 | nM | 5.25 |
| CHEMBL235842 | — | Ki | < | 0.2 | nM | - |