Assay Detail
Binding
CHEMBL5045992
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Inhibition of HDAC2-CoREST-LSD1 (unknown origin) using Boc- (Ac)Lys-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by fluorescent assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Optimization of Class I Histone Deacetylase PROTACs Reveals that HDAC1/2 Degradation is Critical to Induce Apoptosis and Cell Arrest in Cancer Cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.75 | 6.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5077287 | — | — | 1 | 6.44 |
| CHEMBL235191 | TACEDINALINE | 3.0 | 1 | 6.21 |
| CHEMBL5084955 | — | — | 1 | 6.09 |
| CHEMBL5077743 | — | — | 1 | 5.46 |
| CHEMBL5080755 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5077287 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL235191 | TACEDINALINE | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5084955 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5077743 | — | IC50 | = | 3460.0 | nM | 5.46 |
| CHEMBL5080755 | — | IC50 | = | 28380.0 | nM | 4.55 |