Assay Detail
Functional
CHEMBL656170
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In vitro agonistic activity 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 | 8.40 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL422088 | — | — | 1 | 9.40 |
| CHEMBL133896 | — | — | 1 | 9.15 |
| CHEMBL130232 | — | — | 1 | 9.10 |
| CHEMBL133915 | — | — | 1 | 8.89 |
| CHEMBL130231 | — | — | 1 | 8.57 |
| CHEMBL132568 | — | — | 1 | 8.57 |
| CHEMBL337393 | — | — | 1 | 8.57 |
| CHEMBL131826 | — | — | 1 | 8.39 |
| CHEMBL130374 | — | — | 1 | 8.33 |
| CHEMBL111217 | — | — | 1 | 8.19 |
| CHEMBL130317 | — | — | 1 | 8.13 |
| CHEMBL424269 | — | — | 1 | 8.13 |
| CHEMBL75133 | IRX-4204 | 2.0 | 1 | 8.07 |
| CHEMBL335242 | — | — | 1 | 7.91 |
| CHEMBL131122 | — | — | 1 | 7.82 |
| CHEMBL424639 | — | — | 1 | 7.79 |
| CHEMBL288436 | — | — | 1 | 7.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL422088 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL133896 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL130232 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL133915 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL130231 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL132568 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL337393 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL131826 | — | EC50 | = | 4.1 | nM | 8.39 |
| CHEMBL130374 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL111217 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL130317 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL424269 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL75133 | IRX-4204 | EC50 | = | 8.6 | nM | 8.07 |
| CHEMBL335242 | — | EC50 | = | 12.2 | nM | 7.91 |
| CHEMBL131122 | — | EC50 | = | 15.1 | nM | 7.82 |
| CHEMBL424639 | — | EC50 | = | 16.3 | nM | 7.79 |
| CHEMBL288436 | — | EC50 | = | 18.6 | nM | 7.73 |