Assay Detail
Functional
CHEMBL1114666
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Agonist activity at glucocorticoid receptor in human fibroblast assessed as inhibition of IL-1-beta-induced IL6 production treated 1 hr before IL1-beta challenge measured after 24 hrs by transrepression assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| 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 | 7.24 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 8.52 |
| CHEMBL1094208 | 1-(2,3-DICHLOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | — | 1 | 7.72 |
| CHEMBL1094231 | 1-(3-CHLORO-4-FLUOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | — | 1 | 7.03 |
| CHEMBL1094514 | — | — | 1 | 7.03 |
| CHEMBL1096467 | — | — | 1 | 6.95 |
| CHEMBL1094209 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1094208 | 1-(2,3-DICHLOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1094231 | 1-(3-CHLORO-4-FLUOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL1094514 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL1096467 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL1094209 | — | EC50 | = | 627.0 | nM | 6.20 |