Assay Detail
Binding
CHEMBL5316724
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Agonist activity at human GAL4-fused RXRgamma LBD expressed in human HEK293T cells cotransfected with pFR-Luc and pRL-SV40 assessed as increase in luciferase activity incubated for 16 hrs by Dual-Glo luciferase assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Rational Design of a New RXR Agonist Scaffold Enabling Single-Subtype Preference for RXRα, RXRβ, and RXRγ.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 5.16 | 5.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5398107 | — | — | 1 | 5.60 |
| CHEMBL5415478 | — | — | 1 | 5.58 |
| CHEMBL5415488 | — | — | 1 | 5.55 |
| CHEMBL5430265 | — | — | 1 | 5.50 |
| CHEMBL5436493 | — | — | 1 | 5.40 |
| CHEMBL5417534 | — | — | 1 | 5.30 |
| CHEMBL5412916 | — | — | 1 | 5.30 |
| CHEMBL5395485 | — | — | 1 | 5.30 |
| CHEMBL5411747 | — | — | 1 | 5.10 |
| CHEMBL5423689 | — | — | 1 | 4.97 |
| CHEMBL5397808 | — | — | 1 | 4.96 |
| CHEMBL5420687 | — | — | 1 | 4.96 |
| CHEMBL5420641 | — | — | 1 | 4.89 |
| CHEMBL5416412 | — | — | 1 | 4.85 |
| CHEMBL5433310 | — | — | 1 | 4.85 |
| CHEMBL1545045 | VALERENIC ACID | — | 1 | 4.37 |
| CHEMBL5411285 | — | — | 1 | - |
| CHEMBL5415007 | — | — | 1 | - |
| CHEMBL5403049 | — | — | 1 | - |
| CHEMBL4864441 | — | — | 1 | - |
| CHEMBL5418573 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5398107 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5415478 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5415488 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5430265 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5436493 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5417534 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5412916 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5395485 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5411747 | — | EC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5423689 | — | EC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL5397808 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL5420687 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL5420641 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL5416412 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL5433310 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL1545045 | VALERENIC ACID | EC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL5411285 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5415007 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5403049 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4864441 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5418573 | — | EC50 | > | 100000.0 | nM | - |