Assay Detail
ADMET
CHEMBL4686879
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Agonist activity at human RXRalpha/LXRalpha expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha (CHEMBL3430879) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of new LXRβ agonists as glioblastoma inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 9.04 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4764328 | — | — | 1 | 10.10 |
| CHEMBL62136 | T091317 | — | 1 | 10.01 |
| CHEMBL4756418 | — | — | 1 | 9.84 |
| CHEMBL4745005 | — | — | 1 | 9.79 |
| CHEMBL4764838 | — | — | 1 | 9.76 |
| CHEMBL4747448 | — | — | 1 | 9.67 |
| CHEMBL4749385 | — | — | 1 | 9.60 |
| CHEMBL4762546 | — | — | 1 | 9.57 |
| CHEMBL4797369 | — | — | 1 | 9.57 |
| CHEMBL4757761 | — | — | 1 | 9.56 |
| CHEMBL4760781 | — | — | 1 | 9.56 |
| CHEMBL4755317 | — | — | 1 | 9.43 |
| CHEMBL59030 | — | — | 1 | 9.40 |
| CHEMBL456237 | LXR-623 | 1.0 | 1 | 9.37 |
| CHEMBL4757158 | — | — | 1 | 9.15 |
| CHEMBL4791199 | — | — | 1 | 9.07 |
| CHEMBL4748480 | — | — | 1 | 9.03 |
| CHEMBL4777240 | — | — | 1 | 9.03 |
| CHEMBL4780872 | — | — | 1 | 8.97 |
| CHEMBL4764539 | — | — | 1 | 8.93 |
| CHEMBL4762542 | — | — | 1 | 8.76 |
| CHEMBL4781683 | — | — | 1 | 8.71 |
| CHEMBL4759393 | — | — | 1 | 8.71 |
| CHEMBL593241 | — | — | 1 | 5.22 |
| CHEMBL551248 | — | — | 1 | 5.07 |
| CHEMBL4791235 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4764328 | — | EC50 | = | 0.08 | nM | 10.10 |
| CHEMBL62136 | T091317 | EC50 | = | 0.098 | nM | 10.01 |
| CHEMBL4756418 | — | EC50 | = | 0.145 | nM | 9.84 |
| CHEMBL4745005 | — | EC50 | = | 0.161 | nM | 9.79 |
| CHEMBL4764838 | — | EC50 | = | 0.174 | nM | 9.76 |
| CHEMBL4747448 | — | EC50 | = | 0.214 | nM | 9.67 |
| CHEMBL4749385 | — | EC50 | = | 0.251 | nM | 9.60 |
| CHEMBL4762546 | — | EC50 | = | 0.27 | nM | 9.57 |
| CHEMBL4797369 | — | EC50 | = | 0.27 | nM | 9.57 |
| CHEMBL4757761 | — | EC50 | = | 0.274 | nM | 9.56 |
| CHEMBL4760781 | — | EC50 | = | 0.277 | nM | 9.56 |
| CHEMBL4755317 | — | EC50 | = | 0.372 | nM | 9.43 |
| CHEMBL59030 | — | EC50 | = | 0.401 | nM | 9.40 |
| CHEMBL456237 | LXR-623 | EC50 | = | 0.431 | nM | 9.37 |
| CHEMBL4757158 | — | EC50 | = | 0.708 | nM | 9.15 |
| CHEMBL4791199 | — | EC50 | = | 0.843 | nM | 9.07 |
| CHEMBL4748480 | — | EC50 | = | 0.928 | nM | 9.03 |
| CHEMBL4777240 | — | EC50 | = | 0.94 | nM | 9.03 |
| CHEMBL4780872 | — | EC50 | = | 1.071 | nM | 8.97 |
| CHEMBL4764539 | — | EC50 | = | 1.176 | nM | 8.93 |
| CHEMBL4762542 | — | EC50 | = | 1.746 | nM | 8.76 |
| CHEMBL4781683 | — | EC50 | = | 1.954 | nM | 8.71 |
| CHEMBL4759393 | — | EC50 | = | 1.968 | nM | 8.71 |
| CHEMBL593241 | — | EC50 | = | 5960.0 | nM | 5.22 |
| CHEMBL551248 | — | EC50 | = | 8440.0 | nM | 5.07 |
| CHEMBL4791235 | — | EC50 | > | 10.0 | nM | - |