Assay Detail
Functional
CHEMBL1114668
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at glucocorticoid receptor in human MDA-kb2 cells transfected with MMTV-LUC assessed as induction of MMTV-LTR/promoter linked LUC gene by luciferase transactivation assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA-kb2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
5-Functionalized indazoles as glucocorticoid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 6.56 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.26 |
| CHEMBL1094208 | 1-(2,3-DICHLOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | — | 1 | 6.46 |
| CHEMBL1094231 | 1-(3-CHLORO-4-FLUOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | — | 1 | 5.96 |
| CHEMBL1094209 | — | — | 1 | - |
| CHEMBL1096467 | — | — | 1 | - |
| CHEMBL1094514 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1094208 | 1-(2,3-DICHLOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1094231 | 1-(3-CHLORO-4-FLUOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1094209 | — | EC50 | - | — | - | |
| CHEMBL1096467 | — | EC50 | - | — | - | |
| CHEMBL1094514 | — | EC50 | - | — | - |