Assay Detail
Binding
CHEMBL1049548
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Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Huh-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.05 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL62136 | T091317 | — | 1 | 6.77 |
| CHEMBL593267 | — | — | 1 | 6.20 |
| CHEMBL591582 | — | — | 1 | 5.80 |
| CHEMBL456237 | LXR-623 | 1.0 | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL62136 | T091317 | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL593267 | — | EC50 | = | 630.0 | nM | 6.20 |
| CHEMBL591582 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL456237 | LXR-623 | EC50 | = | 3670.0 | nM | 5.43 |