Assay Detail
Binding
CHEMBL4840200
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 CCL2-promoter luciferase plasmid construct assessed as reduction in IL-1 beta induced inflammation 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 |
|---|---|---|---|
| IC50 | 34 | 7.42 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4863316 | — | — | 1 | 9.80 |
| CHEMBL4877227 | — | — | 1 | 9.70 |
| CHEMBL312627 | — | — | 1 | 9.60 |
| CHEMBL4850526 | — | — | 1 | 8.70 |
| CHEMBL4857046 | — | — | 1 | 8.50 |
| CHEMBL311662 | — | — | 1 | 8.30 |
| CHEMBL233390 | — | — | 1 | 8.30 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.20 |
| CHEMBL420767 | — | — | 1 | 8.20 |
| CHEMBL4872787 | — | — | 1 | 8.20 |
| CHEMBL4855992 | — | — | 1 | 8.10 |
| CHEMBL4868414 | — | — | 1 | 8.10 |
| CHEMBL79807 | — | — | 1 | 8.00 |
| CHEMBL313062 | — | — | 1 | 7.80 |
| CHEMBL389621 | HYDROCORTISONE | 4.0 | 1 | 7.60 |
| CHEMBL4846557 | — | — | 1 | 7.50 |
| CHEMBL4875267 | — | — | 1 | 7.40 |
| CHEMBL81591 | — | — | 1 | 7.40 |
| CHEMBL312041 | — | — | 1 | 7.40 |
| CHEMBL4853394 | — | — | 1 | 7.20 |
| CHEMBL4856145 | — | — | 1 | 7.10 |
| CHEMBL4872009 | — | — | 1 | 7.00 |
| CHEMBL4871954 | — | — | 1 | 6.80 |
| CHEMBL4866467 | — | — | 1 | 6.60 |
| CHEMBL4867686 | — | — | 1 | 6.60 |
| CHEMBL4860401 | — | — | 1 | 6.40 |
| CHEMBL4864367 | — | — | 1 | 6.30 |
| CHEMBL4876447 | — | — | 1 | 6.30 |
| CHEMBL4850324 | — | — | 1 | 6.20 |
| CHEMBL4845663 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4863316 | — | IC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL4877227 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL312627 | — | IC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL4850526 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4857046 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL311662 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL233390 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL384467 | DEXAMETHASONE | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL420767 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4872787 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4855992 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4868414 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL79807 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL313062 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL389621 | HYDROCORTISONE | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4846557 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL312041 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL81591 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4875267 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4853394 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4856145 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4872009 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4871954 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4866467 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4867686 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4860401 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4864367 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4876447 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4850324 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4845663 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4868293 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4871994 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4867877 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4850604 | — | IC50 | = | 2511.89 | nM | 5.60 |