Assay Detail
ADMET
CHEMBL4198902
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human recombinant C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (95 to 489 residues) expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) (CHEMBL2111363) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.73 | 5.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4217821 | — | — | 1 | 5.87 |
| CHEMBL4212186 | — | — | 1 | 5.68 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 5.65 |
| CHEMBL4212866 | — | — | 1 | - |
| CHEMBL4214699 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4217821 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4212186 | — | IC50 | = | 2090.0 | nM | 5.68 |
| CHEMBL2018302 | TUBASTATIN A | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL4212866 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4214699 | — | IC50 | > | 20000.0 | nM | - |