Assay Detail
Binding
CHEMBL4818543
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human FLAG-tagged HDAC3 expressed in human HEK293F cells co-expressing His6-tagged SMRT (1 to 899 residues) using Fluor-de-lys substrate as substrate incubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence based assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293F |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.88 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2448576 | — | — | 1 | 9.22 |
| CHEMBL4873847 | — | — | 1 | 8.77 |
| CHEMBL4867665 | — | — | 1 | 8.33 |
| CHEMBL408513 | BELINOSTAT | 4.0 | 1 | 8.14 |
| CHEMBL4879154 | — | — | 1 | 7.75 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.54 |
| CHEMBL4861270 | — | — | 1 | 7.26 |
| CHEMBL4851511 | — | — | 1 | 6.80 |
| CHEMBL4872186 | — | — | 1 | 6.68 |
| CHEMBL4862719 | — | — | 1 | 6.52 |
| CHEMBL4874919 | — | — | 1 | 6.47 |
| CHEMBL4858081 | — | — | 1 | 6.44 |
| CHEMBL4877454 | — | — | 1 | 5.46 |
| CHEMBL4878011 | — | — | 1 | 5.28 |
| CHEMBL4855240 | — | — | 1 | 4.82 |
| CHEMBL4859130 | — | — | 1 | 4.55 |
| CHEMBL4851062 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2448576 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4873847 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4867665 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL408513 | BELINOSTAT | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4879154 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4861270 | — | IC50 | = | 55.2 | nM | 7.26 |
| CHEMBL4851511 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4872186 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4862719 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4874919 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4858081 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4877454 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4878011 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4855240 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4859130 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL4851062 | — | IC50 | > | 50000.0 | nM | - |