Assay Detail
Binding
CHEMBL3855407
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Agonist activity at LXRalpha LBD (unknown origin) fused with Gal4-DNA binding domain expressed in HEK293 cells assessed as modulation of receptor transcription activity by luciferase reporter gene assay
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 |
|---|---|---|---|
| EC50 | 16 | 6.66 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3905741 | — | — | 1 | 7.43 |
| CHEMBL3914727 | — | — | 1 | 7.24 |
| CHEMBL3985591 | — | — | 1 | 7.14 |
| CHEMBL3976470 | — | — | 1 | 7.03 |
| CHEMBL3959681 | — | — | 1 | 6.96 |
| CHEMBL3940521 | — | — | 1 | 6.78 |
| CHEMBL3913348 | — | — | 1 | 6.72 |
| CHEMBL3960195 | — | — | 1 | 6.70 |
| CHEMBL3978980 | — | — | 1 | 6.67 |
| CHEMBL3814206 | — | — | 1 | 6.61 |
| CHEMBL3932169 | — | — | 1 | 6.60 |
| CHEMBL3956923 | — | — | 1 | 6.57 |
| CHEMBL3972392 | — | — | 1 | 6.31 |
| CHEMBL3933543 | — | — | 1 | 6.25 |
| CHEMBL3889601 | — | — | 2 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3905741 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3914727 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3985591 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3976470 | — | EC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3959681 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL3940521 | — | EC50 | = | 166.0 | nM | 6.78 |
| CHEMBL3913348 | — | EC50 | = | 189.0 | nM | 6.72 |
| CHEMBL3960195 | — | EC50 | = | 199.0 | nM | 6.70 |
| CHEMBL3978980 | — | EC50 | = | 214.0 | nM | 6.67 |
| CHEMBL3814206 | — | EC50 | = | 244.0 | nM | 6.61 |
| CHEMBL3932169 | — | EC50 | = | 249.0 | nM | 6.60 |
| CHEMBL3956923 | — | EC50 | = | 271.0 | nM | 6.57 |
| CHEMBL3972392 | — | EC50 | = | 491.0 | nM | 6.31 |
| CHEMBL3933543 | — | EC50 | = | 567.0 | nM | 6.25 |
| CHEMBL3889601 | — | EC50 | = | 1376.0 | nM | 5.86 |
| CHEMBL3889601 | — | EC50 | = | 2241.0 | nM | 5.65 |