Assay Detail
Functional
CHEMBL894377
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Agonist activity at GAL-linked human LXRalpha expressed in THP1 cells assessed as stimulation of coactivator recruitment by FRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 5.98 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL242842 | — | — | 1 | 7.16 |
| CHEMBL59030 | — | — | 1 | 7.01 |
| CHEMBL242840 | — | — | 1 | 6.75 |
| CHEMBL243927 | — | — | 1 | 6.16 |
| CHEMBL243719 | — | — | 1 | 6.05 |
| CHEMBL243718 | — | — | 1 | 6.05 |
| CHEMBL242622 | — | — | 1 | 5.85 |
| CHEMBL242620 | — | — | 1 | 5.85 |
| CHEMBL243494 | — | — | 1 | 5.82 |
| CHEMBL427697 | — | — | 1 | 5.80 |
| CHEMBL243063 | — | — | 1 | 5.72 |
| CHEMBL429818 | — | — | 1 | 5.68 |
| CHEMBL387997 | — | — | 1 | 5.64 |
| CHEMBL395491 | — | — | 1 | 5.62 |
| CHEMBL243531 | — | — | 1 | 5.41 |
| CHEMBL442416 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL242842 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL59030 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL242840 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL243927 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL243719 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL243718 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL242622 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL242620 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL243494 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL427697 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL243063 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL429818 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL387997 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL395491 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL243531 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL442416 | — | EC50 | = | 6700.0 | nM | 5.17 |