Assay Detail
Binding
CHEMBL5100168
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis
24
Total Activities
24
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
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.29 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4170198 | — | — | 1 | 8.30 |
| CHEMBL5187433 | — | — | 1 | 7.89 |
| CHEMBL1213492 | GIVINOSTAT | 4.0 | 1 | 7.46 |
| CHEMBL5199849 | — | — | 1 | 7.18 |
| CHEMBL5189808 | — | — | 1 | 7.11 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.00 |
| CHEMBL5209024 | — | — | 1 | 6.80 |
| CHEMBL4173361 | — | — | 1 | 6.60 |
| CHEMBL5180418 | — | — | 1 | 6.51 |
| CHEMBL5194945 | — | — | 1 | 6.24 |
| CHEMBL5184839 | — | — | 1 | 6.11 |
| CHEMBL5190554 | — | — | 1 | 6.03 |
| CHEMBL5189667 | — | — | 1 | 5.93 |
| CHEMBL5187865 | — | — | 1 | 5.84 |
| CHEMBL5183285 | — | — | 1 | 5.82 |
| CHEMBL5201168 | — | — | 1 | 5.76 |
| CHEMBL5188109 | — | — | 1 | 5.76 |
| CHEMBL4066043 | — | — | 1 | 5.68 |
| CHEMBL5204510 | — | — | 1 | 5.63 |
| CHEMBL5187265 | — | — | 1 | 5.62 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 5.60 |
| CHEMBL5188237 | — | — | 1 | 5.51 |
| CHEMBL5197066 | — | — | 1 | 5.46 |
| CHEMBL5170634 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4170198 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5187433 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1213492 | GIVINOSTAT | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5199849 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5189808 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5209024 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4173361 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL5180418 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5194945 | — | IC50 | = | 573.0 | nM | 6.24 |
| CHEMBL5184839 | — | IC50 | = | 771.0 | nM | 6.11 |
| CHEMBL5190554 | — | IC50 | = | 938.0 | nM | 6.03 |
| CHEMBL5189667 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL5187865 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL5183285 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5201168 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL5188109 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL4066043 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5204510 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL5187265 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL2018302 | TUBASTATIN A | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL5188237 | — | IC50 | = | 3110.0 | nM | 5.51 |
| CHEMBL5197066 | — | IC50 | = | 3470.0 | nM | 5.46 |
| CHEMBL5170634 | — | IC50 | = | 8010.0 | nM | 5.10 |