Assay Detail
Binding
CHEMBL4158091
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay
49
Total Activities
49
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
Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 49 | 6.99 | 10.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545280 | EFATUTAZONE | 2.0 | 1 | 10.42 |
| CHEMBL4172322 | — | — | 1 | 8.36 |
| CHEMBL4170594 | — | — | 1 | 7.92 |
| CHEMBL4163066 | — | — | 1 | 7.68 |
| CHEMBL4164018 | — | — | 1 | 7.68 |
| CHEMBL4171548 | — | — | 1 | 7.66 |
| CHEMBL4160620 | — | — | 1 | 7.64 |
| CHEMBL4169279 | — | — | 1 | 7.64 |
| CHEMBL4167873 | — | — | 1 | 7.41 |
| CHEMBL4176512 | — | — | 1 | 7.40 |
| CHEMBL4165852 | — | — | 1 | 7.40 |
| CHEMBL4164423 | — | — | 1 | 7.39 |
| CHEMBL4169557 | — | — | 1 | 7.37 |
| CHEMBL2104753 | RIVOGLITAZONE | 3.0 | 1 | 7.37 |
| CHEMBL4168263 | — | — | 1 | 7.25 |
| CHEMBL4174671 | — | — | 1 | 7.21 |
| CHEMBL4162908 | — | — | 1 | 7.19 |
| CHEMBL4162757 | — | — | 1 | 7.19 |
| CHEMBL4164753 | — | — | 1 | 7.17 |
| CHEMBL4176105 | — | — | 1 | 7.10 |
| CHEMBL4163237 | — | — | 1 | 7.07 |
| CHEMBL4170847 | — | — | 1 | 7.06 |
| CHEMBL4175728 | — | — | 1 | 7.04 |
| CHEMBL4160935 | — | — | 1 | 7.02 |
| CHEMBL4176459 | — | — | 1 | 6.95 |
| CHEMBL4168205 | — | — | 1 | 6.93 |
| CHEMBL4172725 | — | — | 1 | 6.91 |
| CHEMBL4161407 | — | — | 1 | 6.90 |
| CHEMBL4164769 | — | — | 1 | 6.87 |
| CHEMBL4164442 | — | — | 1 | 6.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545280 | EFATUTAZONE | EC50 | = | 0.038 | nM | 10.42 |
| CHEMBL4172322 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4170594 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4163066 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4164018 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4171548 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4160620 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4169279 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4167873 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4176512 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4165852 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4164423 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2104753 | RIVOGLITAZONE | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4169557 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4168263 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4174671 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4162908 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4162757 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4164753 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4176105 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4163237 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4170847 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4175728 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4160935 | — | EC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4176459 | — | EC50 | = | 113.0 | nM | 6.95 |
| CHEMBL4168205 | — | EC50 | = | 118.0 | nM | 6.93 |
| CHEMBL4172725 | — | EC50 | = | 122.0 | nM | 6.91 |
| CHEMBL4161407 | — | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4164769 | — | EC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4164442 | — | EC50 | = | 139.0 | nM | 6.86 |
| CHEMBL4172668 | — | EC50 | = | 143.0 | nM | 6.84 |
| CHEMBL4173286 | — | EC50 | = | 188.0 | nM | 6.73 |
| CHEMBL4164824 | — | EC50 | = | 201.0 | nM | 6.70 |
| CHEMBL4161352 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4169731 | — | EC50 | = | 235.0 | nM | 6.63 |
| CHEMBL4166201 | — | EC50 | = | 299.0 | nM | 6.52 |
| CHEMBL4159072 | — | EC50 | = | 307.0 | nM | 6.51 |
| CHEMBL4167211 | — | EC50 | = | 318.0 | nM | 6.50 |
| CHEMBL4171415 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4175074 | — | EC50 | = | 356.0 | nM | 6.45 |
| CHEMBL4161305 | — | EC50 | = | 391.0 | nM | 6.41 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 396.0 | nM | 6.40 |
| CHEMBL4159730 | — | EC50 | = | 395.0 | nM | 6.40 |
| CHEMBL4169333 | — | EC50 | = | 474.0 | nM | 6.32 |
| CHEMBL4176819 | — | EC50 | = | 797.0 | nM | 6.10 |
| CHEMBL4167709 | — | EC50 | = | 845.0 | nM | 6.07 |
| CHEMBL4176058 | — | EC50 | = | 1326.0 | nM | 5.88 |
| CHEMBL4159798 | — | EC50 | = | 1434.0 | nM | 5.84 |
| CHEMBL4161693 | — | EC50 | = | 6094.0 | nM | 5.21 |