Assay Detail
Binding
CHEMBL3877340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf21 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.89 | 6.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3917405 | — | — | 1 | 6.65 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.51 |
| CHEMBL3945293 | — | — | 1 | 5.63 |
| CHEMBL3942555 | — | — | 1 | 5.62 |
| CHEMBL3980203 | — | — | 1 | 5.51 |
| CHEMBL3951291 | — | — | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3917405 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL3945293 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL3942555 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3980203 | — | IC50 | = | 3090.0 | nM | 5.51 |
| CHEMBL3951291 | — | IC50 | = | 4070.0 | nM | 5.39 |