Assay Detail
Binding
CHEMBL3052673
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of Homo sapiens (human) PPARgamma assessed as luciferase activity by reporter gene assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The application of comparative molecular field analysis for the design of -anilino substituted-3-phenyl propanoic acids as novel PPAR/ dual ligands
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 31 | 7.40 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL358379 | — | — | 1 | 10.00 |
| CHEMBL147384 | — | — | 1 | 9.90 |
| CHEMBL107367 | FARGLITAZAR | 2.0 | 1 | 9.47 |
| CHEMBL356382 | — | — | 1 | 9.22 |
| CHEMBL106666 | GW7845 | — | 1 | 9.15 |
| CHEMBL2237300 | — | — | 1 | 9.00 |
| CHEMBL358325 | — | — | 1 | 8.89 |
| CHEMBL147090 | — | — | 1 | 8.68 |
| CHEMBL81248 | — | — | 1 | 8.52 |
| CHEMBL77502 | LY-510929 | — | 1 | 8.40 |
| CHEMBL2237301 | — | — | 1 | 8.40 |
| CHEMBL104850 | — | — | 1 | 8.33 |
| CHEMBL166637 | — | — | 1 | 7.96 |
| CHEMBL2237304 | — | — | 1 | 7.70 |
| CHEMBL104246 | — | — | 1 | 7.62 |
| CHEMBL2237303 | — | — | 1 | 7.50 |
| CHEMBL355695 | — | — | 1 | 7.36 |
| CHEMBL86658 | — | — | 1 | 6.77 |
| CHEMBL321634 | — | — | 1 | 6.62 |
| CHEMBL167430 | — | — | 1 | 6.48 |
| CHEMBL412371 | — | — | 1 | 6.42 |
| CHEMBL24038 | RAGAGLITAZAR | 2.0 | 1 | 6.24 |
| CHEMBL2237302 | — | — | 1 | 6.20 |
| CHEMBL87307 | — | — | 1 | 6.05 |
| CHEMBL421729 | — | — | 1 | 5.77 |
| CHEMBL328099 | — | — | 1 | 5.66 |
| CHEMBL314483 | — | — | 1 | 5.57 |
| CHEMBL87380 | — | — | 1 | 5.51 |
| CHEMBL86657 | — | — | 1 | 5.48 |
| CHEMBL89152 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL358379 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL147384 | — | EC50 | = | 0.1259 | nM | 9.90 |
| CHEMBL107367 | FARGLITAZAR | EC50 | = | 0.3388 | nM | 9.47 |
| CHEMBL356382 | — | EC50 | = | 0.6026 | nM | 9.22 |
| CHEMBL106666 | GW7845 | EC50 | = | 0.7079 | nM | 9.15 |
| CHEMBL2237300 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL358325 | — | EC50 | = | 1.288 | nM | 8.89 |
| CHEMBL147090 | — | EC50 | = | 2.089 | nM | 8.68 |
| CHEMBL81248 | — | EC50 | = | 3.02 | nM | 8.52 |
| CHEMBL77502 | LY-510929 | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL2237301 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL104850 | — | EC50 | = | 4.677 | nM | 8.33 |
| CHEMBL166637 | — | EC50 | = | 10.96 | nM | 7.96 |
| CHEMBL2237304 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL104246 | — | EC50 | = | 23.99 | nM | 7.62 |
| CHEMBL2237303 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL355695 | — | EC50 | = | 43.65 | nM | 7.36 |
| CHEMBL86658 | — | EC50 | = | 169.82 | nM | 6.77 |
| CHEMBL321634 | — | EC50 | = | 239.88 | nM | 6.62 |
| CHEMBL167430 | — | EC50 | = | 331.13 | nM | 6.48 |
| CHEMBL412371 | — | EC50 | = | 380.19 | nM | 6.42 |
| CHEMBL24038 | RAGAGLITAZAR | EC50 | = | 575.44 | nM | 6.24 |
| CHEMBL2237302 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL87307 | — | EC50 | = | 891.25 | nM | 6.05 |
| CHEMBL421729 | — | EC50 | = | 1698.24 | nM | 5.77 |
| CHEMBL328099 | — | EC50 | = | 2187.76 | nM | 5.66 |
| CHEMBL314483 | — | EC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL87380 | — | EC50 | = | 3090.3 | nM | 5.51 |
| CHEMBL86657 | — | EC50 | = | 3311.31 | nM | 5.48 |
| CHEMBL89152 | — | EC50 | = | 4265.8 | nM | 5.37 |
| CHEMBL315048 | — | EC50 | = | 8511.38 | nM | 5.07 |