Assay Detail
ADMET
CHEMBL4811587
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Inhibition of C-terminal FLAG/His-tagged human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf9 cells using ZMAL (Z-Lys(Ac)-AMC) as 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 | ADMET |
| 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 | 6.34 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4868526 | — | — | 1 | 7.22 |
| CHEMBL4849568 | — | — | 1 | 7.00 |
| CHEMBL4854335 | — | — | 1 | 7.00 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.96 |
| CHEMBL4854577 | — | — | 1 | 6.89 |
| CHEMBL4853947 | — | — | 1 | 6.58 |
| CHEMBL4847978 | — | — | 1 | 6.55 |
| CHEMBL4878499 | — | — | 1 | 6.55 |
| CHEMBL4862927 | — | — | 1 | 6.52 |
| CHEMBL4866446 | — | — | 1 | 6.36 |
| CHEMBL2179618 | NEXTURASTAT A | — | 1 | 6.30 |
| CHEMBL4851776 | — | — | 1 | 6.22 |
| CHEMBL4873872 | — | — | 1 | 6.11 |
| CHEMBL4858841 | — | — | 1 | 6.01 |
| CHEMBL4873978 | — | — | 1 | 5.69 |
| CHEMBL4849235 | — | — | 1 | 5.61 |
| CHEMBL4878538 | — | — | 1 | 5.39 |
| CHEMBL4868592 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4868526 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4849568 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4854335 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4854577 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4853947 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4847978 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4878499 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4862927 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4866446 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2179618 | NEXTURASTAT A | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4851776 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4873872 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4858841 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4873978 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL4849235 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL4878538 | — | IC50 | = | 4050.0 | nM | 5.39 |
| CHEMBL4868592 | — | IC50 | = | 8000.0 | nM | 5.10 |