Assay Detail
Binding
CHEMBL4811595
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Inhibition of N-terminal GST-tagged full length human recombinant HDAC6 expressed in baculovirus infected Sf9 cells using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay
18
Total Activities
18
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
Investigation of the in vitro and in vivo efficacy of peptoid-based HDAC inhibitors with dual-stage antiplasmodial activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.27 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4854577 | — | — | 1 | 8.00 |
| CHEMBL2179618 | NEXTURASTAT A | — | 1 | 7.70 |
| CHEMBL4873872 | — | — | 1 | 7.70 |
| CHEMBL4854335 | — | — | 1 | 7.52 |
| CHEMBL4851776 | — | — | 1 | 7.52 |
| CHEMBL4847978 | — | — | 1 | 7.52 |
| CHEMBL4853947 | — | — | 1 | 7.40 |
| CHEMBL4873978 | — | — | 1 | 7.40 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.30 |
| CHEMBL4849235 | — | — | 1 | 7.30 |
| CHEMBL4868526 | — | — | 1 | 7.22 |
| CHEMBL4878499 | — | — | 1 | 7.22 |
| CHEMBL4849568 | — | — | 1 | 7.22 |
| CHEMBL4866446 | — | — | 1 | 7.16 |
| CHEMBL4878538 | — | — | 1 | 6.89 |
| CHEMBL4868592 | — | — | 1 | 6.64 |
| CHEMBL4862927 | — | — | 1 | 6.60 |
| CHEMBL4858841 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4854577 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2179618 | NEXTURASTAT A | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4873872 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4854335 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4851776 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4847978 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4853947 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4873978 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4849235 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4868526 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4878499 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4849568 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4866446 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4878538 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4868592 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4862927 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4858841 | — | IC50 | = | 270.0 | nM | 6.57 |