Assay Detail
Binding
CHEMBL5128934
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as equilibrium inhibition constant (Ki,1) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay
3
Total Activities
3
Compounds Tested
1
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
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 6.42 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4526892 | — | — | 1 | 7.60 |
| CHEMBL5195471 | — | — | 1 | 6.16 |
| CHEMBL27759 | ENTINOSTAT | 3.0 | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4526892 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL5195471 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL27759 | ENTINOSTAT | Ki | = | 3200.0 | nM | 5.50 |