Assay Detail
Binding
CHEMBL4150585
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Inhibition of full length human recombinant HDAC1 expressed in baculovirus expression system using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay
18
Total Activities
18
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 Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.07 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4159366 | — | — | 1 | 7.75 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.40 |
| CHEMBL4160840 | — | — | 1 | 6.80 |
| CHEMBL4167286 | — | — | 1 | 6.60 |
| CHEMBL4175555 | — | — | 1 | 6.60 |
| CHEMBL4160833 | — | — | 1 | 6.46 |
| CHEMBL4167685 | — | — | 1 | 6.42 |
| CHEMBL4165344 | — | — | 1 | 5.96 |
| CHEMBL4170168 | — | — | 1 | 5.77 |
| CHEMBL4164238 | — | — | 1 | 5.68 |
| CHEMBL4168763 | — | — | 1 | 5.66 |
| CHEMBL4162254 | — | — | 1 | 5.57 |
| CHEMBL4172110 | — | — | 1 | 5.54 |
| CHEMBL4169802 | — | — | 1 | 5.29 |
| CHEMBL4175964 | — | — | 1 | 5.04 |
| CHEMBL4168707 | — | — | 1 | 4.62 |
| CHEMBL4168767 | — | — | 1 | - |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4159366 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4160840 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4167286 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4175555 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4160833 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4167685 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4165344 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4170168 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4164238 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4168763 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4162254 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4172110 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4169802 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4175964 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL4168707 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4168767 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL1078178 | MOMELOTINIB | IC50 | - | — | - |