Assay Detail
Binding
CHEMBL5100169
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Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis
27
Total Activities
24
Compounds Tested
2
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
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.56 | 8.00 |
| IC5 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5187433 | — | — | 3 | 8.00 |
| CHEMBL4170198 | — | — | 1 | 7.96 |
| CHEMBL5189808 | — | — | 1 | 7.89 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 7.85 |
| CHEMBL1213492 | GIVINOSTAT | 4.0 | 1 | 7.85 |
| CHEMBL5199849 | — | — | 1 | 7.80 |
| CHEMBL5201168 | — | — | 1 | 7.77 |
| CHEMBL5184839 | — | — | 1 | 7.75 |
| CHEMBL5190554 | — | — | 1 | 7.75 |
| CHEMBL5209024 | — | — | 1 | 7.70 |
| CHEMBL5180418 | — | — | 1 | 7.70 |
| CHEMBL5183285 | — | — | 1 | 7.70 |
| CHEMBL5197066 | — | — | 1 | 7.68 |
| CHEMBL5194945 | — | — | 1 | 7.62 |
| CHEMBL5189667 | — | — | 1 | 7.58 |
| CHEMBL5188109 | — | — | 1 | 7.57 |
| CHEMBL5204510 | — | — | 1 | 7.57 |
| CHEMBL5187865 | — | — | 1 | 7.57 |
| CHEMBL5188237 | — | — | 1 | 7.42 |
| CHEMBL4173361 | — | — | 1 | 7.40 |
| CHEMBL5170634 | — | — | 2 | 7.38 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.38 |
| CHEMBL5187265 | — | — | 1 | 7.29 |
| CHEMBL4066043 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5187433 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4170198 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5189808 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2018302 | TUBASTATIN A | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1213492 | GIVINOSTAT | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5199849 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5201168 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5184839 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5190554 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5183285 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5209024 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5180418 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5197066 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5194945 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5189667 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5204510 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5188109 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5187865 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5188237 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4173361 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5170634 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5187265 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4066043 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL5187433 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL5187433 | — | IC5 | = | 1.88 | uM | - |
| CHEMBL5170634 | — | IC50 | > | 10000.0 | nM | - |