Assay Detail
Binding
CHEMBL4031302
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Inhibition of C-terminal FLAG His tagged full length human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected sf21 cells using RHKKAc as substrate in presence of ATP
10
Total Activities
10
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
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.78 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4095596 | — | — | 1 | 8.22 |
| CHEMBL4060201 | — | — | 1 | 8.16 |
| CHEMBL4069283 | — | — | 1 | 7.44 |
| CHEMBL4098975 | — | — | 1 | 6.96 |
| CHEMBL4060602 | — | — | 1 | 6.86 |
| CHEMBL4091233 | — | — | 1 | 6.58 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.51 |
| CHEMBL4088824 | — | — | 1 | 6.07 |
| CHEMBL4059703 | — | — | 1 | 5.58 |
| CHEMBL4070306 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4095596 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4060201 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4069283 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4098975 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4060602 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4091233 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL4088824 | — | IC50 | = | 854.0 | nM | 6.07 |
| CHEMBL4059703 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL4070306 | — | IC50 | = | 3540.0 | nM | 5.45 |