Assay Detail
Binding
CHEMBL5128932
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Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as inhibition constant (Ki) 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 | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 7.57 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27759 | ENTINOSTAT | 3.0 | 1 | 8.22 |
| CHEMBL5195471 | — | — | 1 | 7.51 |
| CHEMBL4526892 | — | — | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27759 | ENTINOSTAT | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL5195471 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4526892 | — | Ki | = | 103.0 | nM | 6.99 |