Assay Detail
Functional
CHEMBL1838801
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Agonist activity at GR in human SW1353 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SW1353 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 8.67 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834538 | — | — | 1 | 9.42 |
| CHEMBL1834534 | — | — | 1 | 9.37 |
| CHEMBL1676 | FLUTICASONE FUROATE | 4.0 | 1 | 9.31 |
| CHEMBL1834536 | — | — | 1 | 9.15 |
| CHEMBL1834533 | — | — | 1 | 9.11 |
| CHEMBL1473 | FLUTICASONE PROPIONATE | 4.0 | 1 | 8.96 |
| CHEMBL1834541 | — | — | 1 | 8.76 |
| CHEMBL1834542 | — | — | 1 | 8.73 |
| CHEMBL1834543 | — | — | 1 | 8.55 |
| CHEMBL1834544 | — | — | 1 | 8.53 |
| CHEMBL1834537 | — | — | 1 | 8.41 |
| CHEMBL1834540 | — | — | 1 | 8.13 |
| CHEMBL1834535 | — | — | 1 | 8.06 |
| CHEMBL1370 | BUDESONIDE | 4.0 | 1 | 7.91 |
| CHEMBL3142314 | — | — | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834538 | — | EC50 | = | 0.38 | nM | 9.42 |
| CHEMBL1834534 | — | EC50 | = | 0.43 | nM | 9.37 |
| CHEMBL1676 | FLUTICASONE FUROATE | EC50 | = | 0.49 | nM | 9.31 |
| CHEMBL1834536 | — | EC50 | = | 0.71 | nM | 9.15 |
| CHEMBL1834533 | — | EC50 | = | 0.78 | nM | 9.11 |
| CHEMBL1473 | FLUTICASONE PROPIONATE | EC50 | = | 1.09 | nM | 8.96 |
| CHEMBL1834541 | — | EC50 | = | 1.75 | nM | 8.76 |
| CHEMBL1834542 | — | EC50 | = | 1.87 | nM | 8.73 |
| CHEMBL1834543 | — | EC50 | = | 2.82 | nM | 8.55 |
| CHEMBL1834544 | — | EC50 | = | 2.97 | nM | 8.53 |
| CHEMBL1834537 | — | EC50 | = | 3.93 | nM | 8.41 |
| CHEMBL1834540 | — | EC50 | = | 7.35 | nM | 8.13 |
| CHEMBL1834535 | — | EC50 | = | 8.78 | nM | 8.06 |
| CHEMBL1370 | BUDESONIDE | EC50 | = | 12.4 | nM | 7.91 |
| CHEMBL3142314 | — | EC50 | = | 21.1 | nM | 7.68 |