Assay Detail
Binding
CHEMBL5506672
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His-tagged human HDAC3 (1 to 428 residues)/N-terminal GST tagged human NCOR2 (395 to 489 residues) expressed in baculovirus-infected Sf9 cells using Boc-Lys-(acetyl)-AMC as substrate preincubated with enzyme for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence analysis
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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
HDAC/NAMPT dual inhibitors overcome initial drug-resistance in p53-null leukemia cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.18 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5083249 | — | — | 1 | 9.42 |
| CHEMBL5078985 | — | — | 1 | 9.37 |
| CHEMBL5087431 | — | — | 1 | 9.26 |
| CHEMBL5532146 | — | — | 1 | 9.14 |
| CHEMBL5565699 | — | — | 1 | 8.97 |
| CHEMBL5561465 | — | — | 1 | 8.74 |
| CHEMBL5561596 | — | — | 1 | 8.74 |
| CHEMBL5555272 | — | — | 1 | 8.70 |
| CHEMBL5556752 | — | — | 1 | 8.70 |
| CHEMBL5559648 | — | — | 1 | 8.62 |
| CHEMBL5558823 | — | — | 1 | 8.56 |
| CHEMBL5568033 | — | — | 1 | 8.53 |
| CHEMBL5559070 | — | — | 1 | 8.51 |
| CHEMBL5532078 | — | — | 1 | 8.27 |
| CHEMBL5560853 | — | — | 1 | 8.06 |
| CHEMBL5557716 | — | — | 1 | 7.91 |
| CHEMBL5550071 | — | — | 1 | 7.70 |
| CHEMBL5563379 | — | — | 1 | 7.12 |
| CHEMBL5557041 | — | — | 1 | 7.07 |
| CHEMBL5532409 | — | — | 1 | 7.01 |
| CHEMBL5560674 | — | — | 1 | 6.96 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.88 |
| CHEMBL5558311 | — | — | 1 | 5.81 |
| CHEMBL5560296 | — | — | 1 | - |
| CHEMBL566757 | DAPORINAD | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5083249 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL5078985 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL5087431 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL5532146 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL5565699 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL5561465 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL5561596 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL5555272 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL5556752 | — | IC50 | = | 2.01 | nM | 8.70 |
| CHEMBL5559648 | — | IC50 | = | 2.42 | nM | 8.62 |
| CHEMBL5558823 | — | IC50 | = | 2.74 | nM | 8.56 |
| CHEMBL5568033 | — | IC50 | = | 2.97 | nM | 8.53 |
| CHEMBL5559070 | — | IC50 | = | 3.12 | nM | 8.51 |
| CHEMBL5532078 | — | IC50 | = | 5.43 | nM | 8.27 |
| CHEMBL5560853 | — | IC50 | = | 8.78 | nM | 8.06 |
| CHEMBL5557716 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL5550071 | — | IC50 | = | 20.13 | nM | 7.70 |
| CHEMBL5563379 | — | IC50 | = | 76.8 | nM | 7.12 |
| CHEMBL5557041 | — | IC50 | = | 84.3 | nM | 7.07 |
| CHEMBL5532409 | — | IC50 | = | 97.4 | nM | 7.01 |
| CHEMBL5560674 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL5558311 | — | IC50 | = | 1556.0 | nM | 5.81 |
| CHEMBL5560296 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL566757 | DAPORINAD | IC50 | > | 10000.0 | nM | - |