Assay Detail
Binding
CHEMBL3877341
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 | 21 | 6.57 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3917405 | — | — | 1 | 8.68 |
| CHEMBL3972157 | — | — | 1 | 8.64 |
| CHEMBL3933593 | — | — | 1 | 8.60 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 8.46 |
| CHEMBL3945293 | — | — | 1 | 7.80 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.70 |
| CHEMBL3951291 | — | — | 1 | 7.55 |
| CHEMBL3924682 | — | — | 1 | 7.18 |
| CHEMBL3980203 | — | — | 1 | 6.97 |
| CHEMBL3915689 | — | — | 1 | 6.40 |
| CHEMBL3942555 | — | — | 1 | 6.29 |
| CHEMBL3961053 | — | — | 1 | 6.05 |
| CHEMBL3964125 | — | — | 1 | 5.58 |
| CHEMBL3920872 | — | — | 1 | 5.55 |
| CHEMBL3952364 | — | — | 1 | 5.54 |
| CHEMBL3943650 | — | — | 1 | 5.00 |
| CHEMBL3892860 | — | — | 1 | 4.35 |
| CHEMBL3982857 | — | — | 1 | 4.28 |
| CHEMBL3954183 | — | — | 1 | 4.19 |
| CHEMBL3893970 | — | — | 1 | - |
| CHEMBL3962918 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3917405 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3972157 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3933593 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2018302 | TUBASTATIN A | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3945293 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3951291 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3924682 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3980203 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3915689 | — | IC50 | = | 395.0 | nM | 6.40 |
| CHEMBL3942555 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL3961053 | — | IC50 | = | 899.0 | nM | 6.05 |
| CHEMBL3964125 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3920872 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3952364 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3943650 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3892860 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL3982857 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL3954183 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL3893970 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3962918 | — | IC50 | > | 100000.0 | nM | - |