Assay Detail
Functional
CHEMBL656173
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonist activity against RXR alpha in CV-1 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cercopithecidae |
| Cell Type | CV-1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.25 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130374 | — | — | 1 | 8.72 |
| CHEMBL133915 | — | — | 1 | 8.66 |
| CHEMBL422088 | — | — | 1 | 8.51 |
| CHEMBL130317 | — | — | 1 | 8.44 |
| CHEMBL130232 | — | — | 1 | 8.41 |
| CHEMBL424269 | — | — | 1 | 8.40 |
| CHEMBL337393 | — | — | 1 | 8.34 |
| CHEMBL131826 | — | — | 1 | 8.33 |
| CHEMBL132568 | — | — | 1 | 8.29 |
| CHEMBL133896 | — | — | 1 | 8.28 |
| CHEMBL75133 | IRX-4204 | 2.0 | 1 | 8.22 |
| CHEMBL111217 | — | — | 1 | 8.17 |
| CHEMBL335242 | — | — | 1 | 8.14 |
| CHEMBL131122 | — | — | 1 | 7.97 |
| CHEMBL130231 | — | — | 1 | 7.86 |
| CHEMBL424639 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130374 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL133915 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL422088 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL130317 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL130232 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL424269 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL337393 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL131826 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL132568 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL133896 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL75133 | IRX-4204 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL111217 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL335242 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL131122 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL130231 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL424639 | — | IC50 | = | 57.9 | nM | 7.24 |