Assay Detail
Binding
CHEMBL4031186
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by LPS addition measured after 18 hrs by ELISA
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 9.31 | 10.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1473 | FLUTICASONE PROPIONATE | 4.0 | 1 | 10.36 |
| CHEMBL4061359 | — | — | 1 | 10.14 |
| CHEMBL4104286 | — | — | 1 | 10.10 |
| CHEMBL4086388 | — | — | 1 | 10.00 |
| CHEMBL4094154 | — | — | 1 | 9.88 |
| CHEMBL4072756 | AZD-5423 | 2.0 | 1 | 9.80 |
| CHEMBL3666813 | — | — | 1 | 9.77 |
| CHEMBL4070346 | — | — | 1 | 9.60 |
| CHEMBL4066614 | — | — | 1 | 9.49 |
| CHEMBL3666814 | — | — | 1 | 9.42 |
| CHEMBL3666807 | VELSECORAT | 2.0 | 1 | 9.37 |
| CHEMBL3915997 | — | — | 1 | 9.30 |
| CHEMBL3666805 | — | — | 1 | 9.27 |
| CHEMBL4098641 | — | — | 1 | 9.21 |
| CHEMBL3666810 | — | — | 1 | 9.20 |
| CHEMBL3666806 | — | — | 1 | 9.18 |
| CHEMBL3666820 | — | — | 1 | 9.03 |
| CHEMBL4096557 | — | — | 1 | 8.96 |
| CHEMBL3666804 | — | — | 1 | 8.85 |
| CHEMBL1370 | BUDESONIDE | 4.0 | 1 | 8.80 |
| CHEMBL4099639 | — | — | 1 | 8.34 |
| CHEMBL4098197 | — | — | 1 | 8.30 |
| CHEMBL4059755 | — | — | 1 | 7.75 |
| CHEMBL4078531 | — | — | 1 | - |
| CHEMBL4083216 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1473 | FLUTICASONE PROPIONATE | IC50 | = | 0.044 | nM | 10.36 |
| CHEMBL4061359 | — | IC50 | = | 0.073 | nM | 10.14 |
| CHEMBL4104286 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL4086388 | — | IC50 | = | 0.101 | nM | 10.00 |
| CHEMBL4094154 | — | IC50 | = | 0.132 | nM | 9.88 |
| CHEMBL4072756 | AZD-5423 | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3666813 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4070346 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4066614 | — | IC50 | = | 0.322 | nM | 9.49 |
| CHEMBL3666814 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL3666807 | VELSECORAT | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL3915997 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3666805 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4098641 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL3666810 | — | IC50 | = | 0.625 | nM | 9.20 |
| CHEMBL3666806 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL3666820 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL4096557 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3666804 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1370 | BUDESONIDE | IC50 | = | 1.57 | nM | 8.80 |
| CHEMBL4099639 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4098197 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4059755 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4078531 | — | IC50 | - | — | - | |
| CHEMBL4083216 | — | IC50 | - | — | - |