Assay Detail
Binding
CHEMBL759728
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In vitro transcription activation on human peroxisome proliferator activated receptor-gamma (PPAR gamma)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 5.97 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293526 | REGLITAZAR | 2.0 | 1 | 7.08 |
| CHEMBL116920 | — | — | 1 | 7.05 |
| CHEMBL118274 | — | — | 1 | 6.82 |
| CHEMBL325844 | — | — | 1 | 6.28 |
| CHEMBL119795 | — | — | 1 | 6.16 |
| CHEMBL119097 | — | — | 1 | 6.08 |
| CHEMBL331388 | — | — | 1 | 5.95 |
| CHEMBL324027 | — | — | 1 | 5.82 |
| CHEMBL117764 | — | — | 1 | 5.69 |
| CHEMBL115463 | — | — | 1 | 5.68 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 5.54 |
| CHEMBL118816 | — | — | 1 | 5.54 |
| CHEMBL117402 | — | — | 1 | 5.52 |
| CHEMBL117796 | — | — | 1 | 5.50 |
| CHEMBL119217 | — | — | 1 | 5.46 |
| CHEMBL118577 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293526 | REGLITAZAR | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL116920 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL118274 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL325844 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL119795 | — | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL119097 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL331388 | — | EC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL324027 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL117764 | — | EC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL115463 | — | EC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL118816 | — | EC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL117402 | — | EC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL117796 | — | EC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL119217 | — | EC50 | = | 3430.0 | nM | 5.46 |
| CHEMBL118577 | — | EC50 | = | 3800.0 | nM | 5.42 |