Assay Detail
Binding
CHEMBL5316718
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Agonist activity at human GAL4-fused RXRalpha 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
20
Total Activities
20
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 | 20 | 5.61 | 6.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5415488 | — | — | 1 | 6.44 |
| CHEMBL5430265 | — | — | 1 | 6.30 |
| CHEMBL5415478 | — | — | 1 | 6.22 |
| CHEMBL5398107 | — | — | 1 | 6.13 |
| CHEMBL5417534 | — | — | 1 | 6.10 |
| CHEMBL5395485 | — | — | 1 | 6.00 |
| CHEMBL5436493 | — | — | 1 | 5.96 |
| CHEMBL5411747 | — | — | 1 | 5.92 |
| CHEMBL5397808 | — | — | 1 | 5.80 |
| CHEMBL5420687 | — | — | 1 | 5.66 |
| CHEMBL5412916 | — | — | 1 | 5.62 |
| CHEMBL5420641 | — | — | 1 | 5.51 |
| CHEMBL5416412 | — | — | 1 | 5.39 |
| CHEMBL4864441 | — | — | 1 | 5.16 |
| CHEMBL5423689 | — | — | 1 | 5.16 |
| CHEMBL5415007 | — | — | 1 | 4.64 |
| CHEMBL1545045 | VALERENIC ACID | — | 1 | 4.57 |
| CHEMBL5411285 | — | — | 1 | 4.37 |
| CHEMBL5403049 | — | — | 1 | - |
| CHEMBL5433310 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5415488 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5430265 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5415478 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5398107 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL5417534 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5395485 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5436493 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5411747 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5397808 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5420687 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5412916 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5420641 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL5416412 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4864441 | — | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5423689 | — | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5415007 | — | EC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL1545045 | VALERENIC ACID | EC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL5411285 | — | EC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL5403049 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5433310 | — | EC50 | > | 100000.0 | nM | - |