Assay Detail
ADMET
CHEMBL4701716
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of human PXR transfected in human HepG2 cells co-transfected with CYP3A4-Luc plasmid incubated for overnight by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| 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
Structure-based amelioration of PXR transactivation in a novel series of macrocyclic allosteric inhibitors of HIV-1 integrase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 5.62 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4753283 | — | — | 1 | 6.00 |
| CHEMBL4454255 | — | — | 1 | 5.24 |
| CHEMBL4743243 | — | — | 1 | - |
| CHEMBL4789249 | — | — | 1 | - |
| CHEMBL4762774 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4753283 | — | EC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4454255 | — | EC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4743243 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL4789249 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL4762774 | — | EC50 | > | 50000.0 | nM | - |