Assay Detail
Functional
CHEMBL998732
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Agonist activity at PPARgamma expressed in human HCA7 cells assessed as induction of peroxisome proliferator response element after 12 hrs by luciferase reporter assay
24
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCA7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Sulindac derivatives that activate the peroxisome proliferator-activated receptor gamma but lack cyclooxygenase inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 6.17 | 7.00 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL457404 | — | — | 1 | 7.00 |
| CHEMBL515204 | — | — | 2 | 7.00 |
| CHEMBL457184 | — | — | 1 | 7.00 |
| CHEMBL457194 | — | — | 1 | 7.00 |
| CHEMBL456768 | — | — | 1 | 6.70 |
| CHEMBL496464 | — | — | 1 | 6.16 |
| CHEMBL18797 | SULINDAC SULFIDE | -1.0 | 1 | 6.10 |
| CHEMBL514405 | — | — | 1 | 6.05 |
| CHEMBL456529 | — | — | 1 | 5.96 |
| CHEMBL457853 | — | — | 1 | 5.96 |
| CHEMBL515823 | — | — | 1 | 5.92 |
| CHEMBL456530 | — | — | 1 | 5.89 |
| CHEMBL456987 | — | — | 1 | 5.82 |
| CHEMBL515831 | — | — | 1 | 5.82 |
| CHEMBL455940 | — | — | 1 | 5.77 |
| CHEMBL456531 | — | — | 1 | 5.72 |
| CHEMBL502126 | — | — | 1 | 5.62 |
| CHEMBL517909 | — | — | 1 | 5.60 |
| CHEMBL505553 | — | — | 1 | - |
| CHEMBL450921 | — | — | 1 | - |
| CHEMBL505097 | — | — | 1 | - |
| CHEMBL496463 | — | — | 1 | - |
| CHEMBL456769 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL457404 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL457184 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL515204 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL457194 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL456768 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL496464 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL18797 | SULINDAC SULFIDE | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL514405 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL456529 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL457853 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL515823 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL456530 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL515831 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL456987 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL455940 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL456531 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL502126 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL517909 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL456769 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL505553 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL450921 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL505097 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL496463 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL515204 | — | Activity | - | — | - |