Assay Detail
ADMET
CHEMBL4818546
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of PXR (unknown origin) expressed in human DPX2 cells co-expressing luciferase gene under control of CYP3A4 promoter assessed as induction of CYP3A4 transcriptional activity incubated for overnight by luminescence based analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | DPX2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 5.56 | 5.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4861270 | — | — | 1 | 5.72 |
| CHEMBL4858081 | — | — | 1 | 5.60 |
| CHEMBL4872186 | — | — | 1 | 5.54 |
| CHEMBL4874919 | — | — | 1 | 5.36 |
| CHEMBL4851511 | — | — | 1 | - |
| CHEMBL4879154 | — | — | 1 | - |
| CHEMBL4867665 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4861270 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4858081 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4872186 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4874919 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4851511 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4879154 | — | EC50 | > | 15000.0 | nM | - |
| CHEMBL4867665 | — | EC50 | > | 30000.0 | nM | - |