Assay Detail
Binding
CHEMBL1049545
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Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| IC50 | 20 | 7.20 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL595689 | — | — | 1 | 9.00 |
| CHEMBL590098 | — | — | 1 | 8.70 |
| CHEMBL600244 | — | — | 1 | 8.66 |
| CHEMBL593739 | — | — | 1 | 8.30 |
| CHEMBL62136 | T091317 | — | 1 | 8.05 |
| CHEMBL589613 | — | — | 1 | 7.96 |
| CHEMBL593267 | — | — | 1 | 7.80 |
| CHEMBL590828 | — | — | 1 | 7.75 |
| CHEMBL591582 | — | — | 1 | 7.75 |
| CHEMBL604259 | — | — | 1 | 7.55 |
| CHEMBL606139 | — | — | 1 | 7.24 |
| CHEMBL602446 | — | — | 1 | 7.21 |
| CHEMBL590584 | — | — | 1 | 7.11 |
| CHEMBL591815 | — | — | 1 | 6.43 |
| CHEMBL593740 | — | — | 1 | 6.23 |
| CHEMBL600851 | — | — | 1 | 6.14 |
| CHEMBL590350 | — | — | 1 | 5.97 |
| CHEMBL606862 | — | — | 1 | 5.54 |
| CHEMBL590586 | — | — | 1 | 5.29 |
| CHEMBL590351 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL595689 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL590098 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL600244 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL593739 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL62136 | T091317 | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL589613 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL593267 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL590828 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL591582 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL604259 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL606139 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL602446 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL590584 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL591815 | — | IC50 | = | 367.0 | nM | 6.43 |
| CHEMBL593740 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL600851 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL590350 | — | IC50 | = | 1076.0 | nM | 5.97 |
| CHEMBL606862 | — | IC50 | = | 2850.0 | nM | 5.54 |
| CHEMBL590586 | — | IC50 | = | 5133.0 | nM | 5.29 |
| CHEMBL590351 | — | IC50 | = | 5294.0 | nM | 5.28 |