Assay Detail
Functional
CHEMBL658541
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro agonist efficacy against PPAR gamma along with 100 nM BRL-49653
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 7.32 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130374 | — | — | 1 | 7.82 |
| CHEMBL131122 | — | — | 1 | 7.54 |
| CHEMBL335242 | — | — | 1 | 7.52 |
| CHEMBL133915 | — | — | 1 | 7.50 |
| CHEMBL130232 | — | — | 1 | 7.44 |
| CHEMBL130317 | — | — | 1 | 7.43 |
| CHEMBL337393 | — | — | 1 | 7.40 |
| CHEMBL422088 | — | — | 1 | 7.34 |
| CHEMBL131826 | — | — | 1 | 7.33 |
| CHEMBL130231 | — | — | 1 | 7.29 |
| CHEMBL75133 | IRX-4204 | 2.0 | 1 | 7.27 |
| CHEMBL132568 | — | — | 1 | 7.23 |
| CHEMBL111217 | — | — | 1 | 7.20 |
| CHEMBL424269 | — | — | 1 | 7.15 |
| CHEMBL424639 | — | — | 1 | 7.11 |
| CHEMBL133896 | — | — | 1 | 7.00 |
| CHEMBL288436 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130374 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL131122 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL335242 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL133915 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL130232 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL130317 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL337393 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL422088 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL131826 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL130231 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL75133 | IRX-4204 | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL132568 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL111217 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL424269 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL424639 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL133896 | — | EC50 | = | 99.0 | nM | 7.00 |
| CHEMBL288436 | — | EC50 | = | 161.0 | nM | 6.79 |