Assay Detail
Binding
CHEMBL3368832
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Inhibition of human HDAC1 expressed in HEK293T cells assessed as aminomethyl coumarin release using Ac-KGLGK(Ac)-MCA) substrate after 30 mins by FLIPR method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Bicyclic tetrapeptides as potent HDAC inhibitors: effect of aliphatic loop position and hydrophobicity on inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.82 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2158745 | — | — | 1 | 9.40 |
| CHEMBL592719 | — | — | 1 | 8.04 |
| CHEMBL589906 | — | — | 1 | 7.60 |
| CHEMBL3309856 | — | — | 1 | 7.60 |
| CHEMBL3309857 | — | — | 1 | 7.60 |
| CHEMBL3309855 | — | — | 1 | 7.51 |
| CHEMBL3309858 | — | — | 1 | 7.43 |
| CHEMBL3356087 | — | — | 1 | 7.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2158745 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL592719 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL589906 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3309856 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3309857 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3309855 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3309858 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3356087 | — | IC50 | = | 43.0 | nM | 7.37 |