Assay Detail
Binding
CHEMBL3784067
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Agonist activity at histidine-tagged ligand binding domain of human RXRalpha expressed in Escherichia coli BL21 (DE3) by luciferase reporter gene assay
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Chiral Dihydrobenzofuran Acids Show Potent Retinoid X Receptor-Nuclear Receptor Related 1 Protein Dimer Activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 7.31 | 8.20 |
| pEC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3781132 | — | — | 1 | 8.20 |
| CHEMBL3780763 | — | — | 1 | 7.70 |
| CHEMBL3779935 | — | — | 1 | 7.60 |
| CHEMBL1023 | BEXAROTENE | 4.0 | 1 | 7.50 |
| CHEMBL3781998 | — | — | 1 | 7.30 |
| CHEMBL3780004 | — | — | 1 | 7.30 |
| CHEMBL3781771 | — | — | 1 | 6.90 |
| CHEMBL3780806 | — | — | 1 | 6.00 |
| CHEMBL3781879 | — | — | 1 | - |
| CHEMBL3781759 | — | — | 1 | - |
| CHEMBL3781374 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3781132 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3780763 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3779935 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1023 | BEXAROTENE | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3781998 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL3780004 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL3781771 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3780806 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3781879 | — | pEC50 | - | — | - | |
| CHEMBL3781759 | — | pEC50 | - | — | - | |
| CHEMBL3781374 | — | pEC50 | - | — | - |