Assay Detail
Binding
CHEMBL2428207
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of glucocorticoid receptor ligand binding domain (unknown origin) transfected in human HeLa cells assessed as activation of NP-1 by GAL4 luciferase reporter gene assay
32
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| 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 | 32 | 7.41 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2426624 | — | — | 2 | 10.00 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.35 |
| CHEMBL2426662 | — | — | 1 | 8.24 |
| CHEMBL2426665 | — | — | 1 | 8.12 |
| CHEMBL2426623 | — | — | 2 | 7.70 |
| CHEMBL2426656 | — | — | 1 | 6.88 |
| CHEMBL2426648 | — | — | 1 | 6.88 |
| CHEMBL2426633 | — | — | 1 | 6.73 |
| CHEMBL2426658 | — | — | 1 | 6.68 |
| CHEMBL2426645 | — | — | 1 | 6.59 |
| CHEMBL2426644 | — | — | 1 | 6.36 |
| CHEMBL1801004 | — | — | 1 | 6.28 |
| CHEMBL2426632 | — | — | 1 | - |
| CHEMBL2426631 | — | — | 1 | - |
| CHEMBL2426630 | — | — | 1 | - |
| CHEMBL2426657 | — | — | 1 | - |
| CHEMBL2426655 | — | — | 1 | - |
| CHEMBL2426654 | — | — | 1 | - |
| CHEMBL2426653 | — | — | 1 | - |
| CHEMBL2426652 | — | — | 1 | - |
| CHEMBL2426651 | — | — | 1 | - |
| CHEMBL2426650 | — | — | 1 | - |
| CHEMBL2426649 | — | — | 1 | - |
| CHEMBL2426646 | — | — | 1 | - |
| CHEMBL2426664 | — | — | 1 | - |
| CHEMBL2426663 | — | — | 1 | - |
| CHEMBL2426661 | — | — | 1 | - |
| CHEMBL2426660 | — | — | 1 | - |
| CHEMBL2426659 | — | — | 1 | - |
| CHEMBL2426647 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2426624 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL2426662 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL2426665 | — | EC50 | = | 7.6 | nM | 8.12 |
| CHEMBL2426623 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2426624 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2426648 | — | EC50 | = | 132.0 | nM | 6.88 |
| CHEMBL2426656 | — | EC50 | = | 132.0 | nM | 6.88 |
| CHEMBL2426633 | — | EC50 | = | 188.0 | nM | 6.73 |
| CHEMBL2426658 | — | EC50 | = | 208.0 | nM | 6.68 |
| CHEMBL2426645 | — | EC50 | = | 256.0 | nM | 6.59 |
| CHEMBL2426644 | — | EC50 | = | 435.0 | nM | 6.36 |
| CHEMBL1801004 | — | EC50 | = | 526.0 | nM | 6.28 |
| CHEMBL2426630 | — | EC50 | - | — | - | |
| CHEMBL2426655 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2426654 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2426653 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2426652 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2426651 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2426650 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2426649 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2426631 | — | EC50 | - | — | - | |
| CHEMBL2426647 | — | EC50 | - | — | - | |
| CHEMBL2426646 | — | EC50 | - | — | - | |
| CHEMBL2426632 | — | EC50 | - | — | - | |
| CHEMBL2426664 | — | EC50 | - | — | - | |
| CHEMBL2426663 | — | EC50 | - | — | - | |
| CHEMBL2426661 | — | EC50 | - | — | - | |
| CHEMBL2426660 | — | EC50 | - | — | - | |
| CHEMBL2426659 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2426657 | — | EC50 | - | — | - | |
| CHEMBL2426623 | — | EC50 | > | 100.0 | nM | - |