Assay Detail
Binding
CHEMBL4840204
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with 3XGRE-promoter luciferase plasmid construct assessed as induction of receptor transactivation by luciferase reporter gene assay
34
Total Activities
34
Compounds Tested
1
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
Potent Anti-Inflammatory, Arylpyrazole-Based Glucocorticoid Receptor Agonists That Do Not Impair Insulin Secretion.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 34 | 6.41 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4853394 | — | — | 1 | 9.40 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.70 |
| CHEMBL4872787 | — | — | 1 | 8.40 |
| CHEMBL4855992 | — | — | 1 | 8.40 |
| CHEMBL4850526 | — | — | 1 | 8.20 |
| CHEMBL4857046 | — | — | 1 | 8.10 |
| CHEMBL311662 | — | — | 1 | 7.80 |
| CHEMBL313062 | — | — | 1 | 7.20 |
| CHEMBL312041 | — | — | 1 | 7.20 |
| CHEMBL420767 | — | — | 1 | 7.20 |
| CHEMBL79807 | — | — | 1 | 7.10 |
| CHEMBL4850604 | — | — | 1 | 7.10 |
| CHEMBL81591 | — | — | 1 | 7.00 |
| CHEMBL233390 | — | — | 1 | 6.90 |
| CHEMBL4867686 | — | — | 1 | 6.90 |
| CHEMBL4863316 | — | — | 1 | 6.60 |
| CHEMBL4850324 | — | — | 1 | 6.50 |
| CHEMBL312627 | — | — | 1 | 6.10 |
| CHEMBL4846557 | — | — | 1 | 5.90 |
| CHEMBL4872009 | — | — | 1 | 5.80 |
| CHEMBL4877227 | — | — | 1 | 5.80 |
| CHEMBL4868414 | — | — | 1 | 5.70 |
| CHEMBL389621 | HYDROCORTISONE | 4.0 | 1 | 5.60 |
| CHEMBL4867877 | — | — | 1 | 5.60 |
| CHEMBL4876447 | — | — | 1 | 5.30 |
| CHEMBL4875267 | — | — | 1 | 5.00 |
| CHEMBL4860401 | — | — | 1 | 5.00 |
| CHEMBL4845663 | — | — | 1 | 5.00 |
| CHEMBL4868293 | — | — | 1 | 5.00 |
| CHEMBL4864367 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4853394 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4872787 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4855992 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4850526 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4857046 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL311662 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL313062 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL312041 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL420767 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL79807 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4850604 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL81591 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL233390 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4867686 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4863316 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4850324 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL312627 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4846557 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4872009 | — | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4877227 | — | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4868414 | — | EC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL389621 | HYDROCORTISONE | EC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4867877 | — | EC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4876447 | — | EC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4875267 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4860401 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4845663 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4868293 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4864367 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4871994 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4856145 | — | EC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL4866467 | — | EC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL4871954 | — | EC50 | = | 100000.0 | nM | 4.00 |