Assay Detail
Binding
CHEMBL3855405
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Displacement of radiolabeled T0901317 from LXRalpha LBD (unknown origin)
17
Total Activities
16
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
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.12 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3905741 | — | — | 1 | 8.15 |
| CHEMBL3959681 | — | — | 1 | 7.70 |
| CHEMBL3914727 | — | — | 1 | 7.66 |
| CHEMBL62136 | T091317 | — | 1 | 7.62 |
| CHEMBL3985591 | — | — | 1 | 7.50 |
| CHEMBL3940521 | — | — | 1 | 7.32 |
| CHEMBL3976470 | — | — | 1 | 7.29 |
| CHEMBL3932169 | — | — | 1 | 7.20 |
| CHEMBL3978980 | — | — | 1 | 7.15 |
| CHEMBL3814206 | — | — | 1 | 7.09 |
| CHEMBL3913348 | — | — | 1 | 7.07 |
| CHEMBL3972392 | — | — | 1 | 6.87 |
| CHEMBL3960195 | — | — | 1 | 6.73 |
| CHEMBL3933543 | — | — | 1 | 6.69 |
| CHEMBL3956923 | — | — | 1 | 6.66 |
| CHEMBL3889601 | — | — | 2 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3905741 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL3959681 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3914727 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL62136 | T091317 | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL3985591 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL3940521 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL3976470 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL3932169 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL3978980 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL3814206 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL3913348 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL3972392 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL3960195 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL3933543 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL3956923 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL3889601 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL3889601 | — | Ki | = | 1365.0 | nM | 5.87 |