Assay Detail
ADMET
CHEMBL3860993
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate after 30 mins by fluorescence analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.07 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3907730 | — | — | 1 | 7.51 |
| CHEMBL3970984 | — | — | 1 | 7.44 |
| CHEMBL3979179 | — | — | 1 | 7.37 |
| CHEMBL3895838 | — | — | 1 | 7.29 |
| CHEMBL3986487 | — | — | 1 | 7.27 |
| CHEMBL3982024 | — | — | 1 | 6.62 |
| CHEMBL3955253 | — | — | 1 | 6.55 |
| CHEMBL3900593 | — | — | 1 | 6.49 |
| CHEMBL3932796 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3907730 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3970984 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3979179 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3895838 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3986487 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3982024 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL3955253 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL3900593 | — | IC50 | = | 322.0 | nM | 6.49 |
| CHEMBL3932796 | — | IC50 | > | 20000.0 | nM | - |