Assay Detail
Functional
CHEMBL894379
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Agonist activity at GAL-linked human LXRbeta expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay
24
Total Activities
24
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 | 24 | 6.53 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL242842 | — | — | 1 | 8.22 |
| CHEMBL59030 | — | — | 1 | 7.57 |
| CHEMBL242840 | — | — | 1 | 7.46 |
| CHEMBL427697 | — | — | 1 | 7.17 |
| CHEMBL242620 | — | — | 1 | 7.12 |
| CHEMBL243927 | — | — | 1 | 7.09 |
| CHEMBL395491 | — | — | 1 | 6.85 |
| CHEMBL243063 | — | — | 1 | 6.82 |
| CHEMBL243719 | — | — | 1 | 6.80 |
| CHEMBL243718 | — | — | 1 | 6.77 |
| CHEMBL242622 | — | — | 1 | 6.70 |
| CHEMBL413795 | — | — | 1 | 6.60 |
| CHEMBL387997 | — | — | 1 | 6.60 |
| CHEMBL429818 | — | — | 1 | 6.33 |
| CHEMBL243494 | — | — | 1 | 6.25 |
| CHEMBL397656 | — | — | 1 | 6.22 |
| CHEMBL243531 | — | — | 1 | 6.10 |
| CHEMBL243493 | — | — | 1 | 6.01 |
| CHEMBL442416 | — | — | 1 | 6.01 |
| CHEMBL389564 | — | — | 1 | 5.47 |
| CHEMBL242841 | — | — | 1 | 5.43 |
| CHEMBL243275 | — | — | 1 | 5.40 |
| CHEMBL243276 | — | — | 1 | 5.11 |
| CHEMBL389563 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL242842 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL59030 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL242840 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL427697 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL242620 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL243927 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL395491 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL243063 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL243719 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL243718 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL242622 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL413795 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL387997 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL429818 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL243494 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL397656 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL243531 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL243493 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL442416 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL389564 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL242841 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL243275 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL243276 | — | EC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL389563 | — | EC50 | > | 10000.0 | nM | - |