Assay Detail
Functional
CHEMBL824648
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro transactivation using receptor transactivation assay against hPPAR gamma
25
Total Activities
25
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
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 5.90 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL166637 | — | — | 1 | 7.96 |
| CHEMBL355695 | — | — | 1 | 7.36 |
| CHEMBL166628 | — | — | 1 | 7.04 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 6.80 |
| CHEMBL86658 | — | — | 1 | 6.77 |
| CHEMBL167430 | — | — | 1 | 6.48 |
| CHEMBL167043 | — | — | 1 | 6.34 |
| CHEMBL166539 | — | — | 1 | 6.31 |
| CHEMBL24038 | RAGAGLITAZAR | 2.0 | 1 | 6.24 |
| CHEMBL167352 | — | — | 1 | 6.12 |
| CHEMBL167963 | — | — | 1 | 6.12 |
| CHEMBL165484 | — | — | 1 | 6.12 |
| CHEMBL408 | TROGLITAZONE | 4.0 | 1 | 6.01 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 6.01 |
| CHEMBL166572 | — | — | 1 | 5.92 |
| CHEMBL168033 | — | — | 1 | 5.77 |
| CHEMBL166687 | — | — | 1 | 5.47 |
| CHEMBL168166 | — | — | 1 | 5.43 |
| CHEMBL167378 | — | — | 1 | 5.01 |
| CHEMBL165539 | — | — | 1 | 4.92 |
| CHEMBL354863 | — | — | 1 | 4.91 |
| CHEMBL167084 | — | — | 1 | 4.90 |
| CHEMBL166408 | — | — | 1 | 4.78 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 4.53 |
| CHEMBL264374 | BEZAFIBRATE | 3.0 | 1 | 4.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL166637 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL355695 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL166628 | — | EC50 | = | 91.0 | nM | 7.04 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL86658 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL167430 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL167043 | — | EC50 | = | 460.0 | nM | 6.34 |
| CHEMBL166539 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL24038 | RAGAGLITAZAR | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL167352 | — | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL167963 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL165484 | — | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL408 | TROGLITAZONE | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL595 | PIOGLITAZONE | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL166572 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL168033 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL166687 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL168166 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL167378 | — | EC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL165539 | — | EC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL354863 | — | EC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL167084 | — | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL166408 | — | EC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 29300.0 | nM | 4.53 |
| CHEMBL264374 | BEZAFIBRATE | EC50 | = | 73500.0 | nM | 4.13 |