Assay Detail
Binding
CHEMBL4347606
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Inhibition of HDAC8 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay
8
Total Activities
8
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
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.65 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4563723 | — | — | 1 | 6.92 |
| CHEMBL4471710 | — | — | 1 | 6.08 |
| CHEMBL4584008 | — | — | 1 | 5.77 |
| CHEMBL4526274 | — | — | 1 | 5.61 |
| CHEMBL4451298 | — | — | 1 | 5.39 |
| CHEMBL4568644 | — | — | 1 | 5.29 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 5.25 |
| CHEMBL4540416 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4563723 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4471710 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4584008 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4526274 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL4451298 | — | IC50 | = | 4070.0 | nM | 5.39 |
| CHEMBL4568644 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4540416 | — | IC50 | = | 14100.0 | nM | 4.85 |