Assay Detail
Binding
CHEMBL5126488
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Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with CCL2-promoter luciferase plasmid construct assessed as reduction in IL-1 beta induced inflammation by luciferase reporter gene assay
20
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | INS-1 832/13 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Stereoisomers of an Aryl Pyrazole Glucocorticoid Receptor Agonist Scaffold Elicit Differing Anti-inflammatory Responses.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.42 | 9.50 |
| %max | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5196090 | — | — | 1 | 9.50 |
| CHEMBL5181366 | — | — | 1 | 9.20 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 2 | 8.90 |
| CHEMBL5199091 | — | — | 1 | 8.30 |
| CHEMBL5200995 | — | — | 1 | 7.80 |
| CHEMBL5196115 | — | — | 1 | 7.70 |
| CHEMBL81591 | — | — | 1 | 7.70 |
| CHEMBL5183169 | — | — | 1 | 7.60 |
| CHEMBL5194382 | — | — | 1 | 7.50 |
| CHEMBL5207591 | — | — | 1 | 7.50 |
| CHEMBL5185246 | — | — | 1 | 7.50 |
| CHEMBL420767 | — | — | 1 | 7.20 |
| CHEMBL5197908 | — | — | 1 | 6.80 |
| CHEMBL389621 | HYDROCORTISONE | 4.0 | 2 | 6.50 |
| CHEMBL5171084 | — | — | 1 | 6.40 |
| CHEMBL5186941 | — | — | 1 | 6.40 |
| CHEMBL5173367 | — | — | 1 | 5.70 |
| CHEMBL5191812 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5196090 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL5181366 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL384467 | DEXAMETHASONE | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL5199091 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL5200995 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL5196115 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL81591 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5183169 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL5207591 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL5185246 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL5194382 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL420767 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5197908 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL389621 | HYDROCORTISONE | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL5186941 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL5171084 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL5173367 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL5191812 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL389621 | HYDROCORTISONE | %max | = | 100.0 | % | - |
| CHEMBL384467 | DEXAMETHASONE | %max | = | 100.0 | % | - |