Assay Detail
Binding
CHEMBL1805665
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Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay
22
Total Activities
22
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
Dimethyl-diphenyl-propanamide derivatives as nonsteroidal dissociated glucocorticoid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 6.89 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.38 |
| CHEMBL1800984 | — | — | 1 | 7.22 |
| CHEMBL1800982 | — | — | 1 | 7.17 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.08 |
| CHEMBL1800985 | — | — | 1 | 7.07 |
| CHEMBL1801006 | — | — | 1 | 6.94 |
| CHEMBL1801008 | — | — | 1 | 6.92 |
| CHEMBL1800981 | — | — | 1 | 6.92 |
| CHEMBL1801009 | — | — | 1 | 6.67 |
| CHEMBL1801012 | — | — | 1 | 6.43 |
| CHEMBL1801004 | — | — | 1 | 6.42 |
| CHEMBL1800983 | — | — | 1 | 6.25 |
| CHEMBL1801013 | — | — | 1 | 6.06 |
| CHEMBL1801011 | — | — | 1 | - |
| CHEMBL1801010 | — | — | 1 | - |
| CHEMBL1801007 | — | — | 1 | - |
| CHEMBL1801005 | — | — | 1 | - |
| CHEMBL1801003 | — | — | 1 | - |
| CHEMBL1800980 | — | — | 1 | - |
| CHEMBL1800979 | — | — | 1 | - |
| CHEMBL1800986 | — | — | 1 | - |
| CHEMBL1800987 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL1800984 | — | EC50 | = | 60.1 | nM | 7.22 |
| CHEMBL1800982 | — | EC50 | = | 67.2 | nM | 7.17 |
| CHEMBL131 | PREDNISOLONE | EC50 | = | 82.7 | nM | 7.08 |
| CHEMBL1800985 | — | EC50 | = | 85.7 | nM | 7.07 |
| CHEMBL1801006 | — | EC50 | = | 114.7 | nM | 6.94 |
| CHEMBL1801008 | — | EC50 | = | 119.0 | nM | 6.92 |
| CHEMBL1800981 | — | EC50 | = | 121.0 | nM | 6.92 |
| CHEMBL1801009 | — | EC50 | = | 216.4 | nM | 6.67 |
| CHEMBL1801012 | — | EC50 | = | 372.1 | nM | 6.43 |
| CHEMBL1801004 | — | EC50 | = | 380.2 | nM | 6.42 |
| CHEMBL1800983 | — | EC50 | = | 555.8 | nM | 6.25 |
| CHEMBL1801013 | — | EC50 | = | 863.4 | nM | 6.06 |
| CHEMBL1801011 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1801010 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1801007 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1801005 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1801003 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1800980 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1800979 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1800986 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1800987 | — | EC50 | > | 10000.0 | nM | - |