Assay Detail
Binding
CHEMBL929248
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay
13
Total Activities
7
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) (CHEMBL2111363) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.45 | 8.05 |
| Ki | 6 | 8.47 | 9.59 |
| Kd | 1 | 8.70 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | 1.0 | 2 | 9.59 |
| CHEMBL430060 | APICIDIN | — | 2 | 8.82 |
| CHEMBL98 | VORINOSTAT | 4.0 | 2 | 8.70 |
| CHEMBL255686 | — | — | 1 | 8.70 |
| CHEMBL260653 | — | — | 2 | 7.64 |
| CHEMBL343448 | ROMIDEPSIN | 4.0 | 2 | 7.60 |
| CHEMBL86537 | SPLITOMICIN | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL430060 | APICIDIN | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL98 | VORINOSTAT | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL255686 | — | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL430060 | APICIDIN | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL260653 | — | Ki | = | 23.1 | nM | 7.64 |
| CHEMBL343448 | ROMIDEPSIN | Ki | = | 24.9 | nM | 7.60 |
| CHEMBL260653 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL343448 | ROMIDEPSIN | IC50 | = | 146.9 | nM | 6.83 |
| CHEMBL86537 | SPLITOMICIN | IC50 | > | 75000.0 | nM | - |
| CHEMBL86537 | SPLITOMICIN | Ki | > | 75000.0 | nM | - |