Assay Detail
Binding
CHEMBL2428211
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL-1beta-induced NF-kappaB dependent E-selectin activation by luciferase reporter gene assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 7.45 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2426665 | — | — | 1 | 9.30 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.96 |
| CHEMBL2426662 | — | — | 1 | 8.40 |
| CHEMBL2426645 | — | — | 1 | 8.00 |
| CHEMBL2426658 | — | — | 1 | 7.82 |
| CHEMBL2426648 | — | — | 1 | 7.72 |
| CHEMBL1801004 | — | — | 1 | 7.68 |
| CHEMBL2426633 | — | — | 1 | 7.68 |
| CHEMBL2426656 | — | — | 1 | 7.31 |
| CHEMBL2426644 | — | — | 1 | 7.24 |
| CHEMBL2426650 | — | — | 1 | 7.11 |
| CHEMBL2426652 | — | — | 1 | 6.84 |
| CHEMBL2426649 | — | — | 1 | 6.73 |
| CHEMBL2426654 | — | — | 1 | 6.71 |
| CHEMBL2426657 | — | — | 1 | 5.98 |
| CHEMBL2426655 | — | — | 1 | 5.74 |
| CHEMBL2426661 | — | — | 1 | - |
| CHEMBL2426660 | — | — | 1 | - |
| CHEMBL2426659 | — | — | 1 | - |
| CHEMBL2426647 | — | — | 1 | - |
| CHEMBL2426663 | — | — | 1 | - |
| CHEMBL2426664 | — | — | 1 | - |
| CHEMBL2426646 | — | — | 1 | - |
| CHEMBL2426651 | — | — | 1 | - |
| CHEMBL2426653 | — | — | 1 | - |
| CHEMBL2426630 | — | — | 1 | - |
| CHEMBL2426631 | — | — | 1 | - |
| CHEMBL2426632 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2426665 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2426662 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2426645 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2426658 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2426648 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1801004 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2426633 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2426656 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2426644 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL2426650 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2426652 | — | EC50 | = | 143.0 | nM | 6.84 |
| CHEMBL2426649 | — | EC50 | = | 185.0 | nM | 6.73 |
| CHEMBL2426654 | — | EC50 | = | 195.0 | nM | 6.71 |
| CHEMBL2426657 | — | EC50 | = | 1047.0 | nM | 5.98 |
| CHEMBL2426655 | — | EC50 | = | 1823.0 | nM | 5.74 |
| CHEMBL2426661 | — | EC50 | - | — | - | |
| CHEMBL2426660 | — | EC50 | - | — | - | |
| CHEMBL2426659 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL2426647 | — | EC50 | - | — | - | |
| CHEMBL2426663 | — | EC50 | - | — | - | |
| CHEMBL2426664 | — | EC50 | - | — | - | |
| CHEMBL2426646 | — | EC50 | - | — | - | |
| CHEMBL2426651 | — | EC50 | - | — | - | |
| CHEMBL2426653 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL2426630 | — | EC50 | - | — | - | |
| CHEMBL2426631 | — | EC50 | - | — | - | |
| CHEMBL2426632 | — | EC50 | - | — | - |