Assay Detail
Binding
CHEMBL1914163
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
32
Total Activities
32
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
Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791826).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 32 | 7.57 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL474189 | — | — | 1 | 8.85 |
| CHEMBL1800985 | — | — | 1 | 8.46 |
| CHEMBL1911270 | — | — | 1 | 8.34 |
| CHEMBL1911278 | — | — | 1 | 8.20 |
| CHEMBL4296682 | — | — | 1 | 8.16 |
| CHEMBL1911273 | — | — | 1 | 8.11 |
| CHEMBL1911150 | — | — | 1 | 8.08 |
| CHEMBL1911156 | — | — | 1 | 7.99 |
| CHEMBL1911279 | — | — | 1 | 7.93 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.84 |
| CHEMBL1911154 | — | — | 1 | 7.70 |
| CHEMBL1911281 | — | — | 1 | 7.69 |
| CHEMBL1911149 | — | — | 1 | 7.67 |
| CHEMBL1911155 | — | — | 1 | 7.64 |
| CHEMBL1911277 | — | — | 1 | 7.59 |
| CHEMBL1911147 | — | — | 1 | 7.58 |
| CHEMBL1911276 | — | — | 1 | 7.54 |
| CHEMBL1911280 | — | — | 1 | 7.54 |
| CHEMBL1801012 | — | — | 1 | 7.53 |
| CHEMBL1911151 | — | — | 1 | 7.53 |
| CHEMBL1911282 | — | — | 1 | 7.47 |
| CHEMBL1911272 | — | — | 1 | 7.47 |
| CHEMBL1911275 | — | — | 1 | 7.19 |
| CHEMBL1911157 | — | — | 1 | 7.14 |
| CHEMBL1911283 | — | — | 1 | 7.13 |
| CHEMBL1911153 | — | — | 1 | 6.97 |
| CHEMBL1911269 | — | — | 1 | 6.80 |
| CHEMBL1911268 | — | — | 1 | 6.67 |
| CHEMBL1911148 | — | — | 1 | 6.45 |
| CHEMBL1911159 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL474189 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1800985 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1911270 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL1911278 | — | EC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4296682 | — | EC50 | = | 6.89 | nM | 8.16 |
| CHEMBL1911273 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL1911150 | — | EC50 | = | 8.3 | nM | 8.08 |
| CHEMBL1911156 | — | EC50 | = | 10.2 | nM | 7.99 |
| CHEMBL1911279 | — | EC50 | = | 11.7 | nM | 7.93 |
| CHEMBL131 | PREDNISOLONE | EC50 | = | 14.4 | nM | 7.84 |
| CHEMBL1911154 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1911281 | — | EC50 | = | 20.6 | nM | 7.69 |
| CHEMBL1911149 | — | EC50 | = | 21.3 | nM | 7.67 |
| CHEMBL1911155 | — | EC50 | = | 22.8 | nM | 7.64 |
| CHEMBL1911277 | — | EC50 | = | 25.6 | nM | 7.59 |
| CHEMBL1911147 | — | EC50 | = | 26.6 | nM | 7.58 |
| CHEMBL1911276 | — | EC50 | = | 28.6 | nM | 7.54 |
| CHEMBL1911280 | — | EC50 | = | 29.2 | nM | 7.54 |
| CHEMBL1801012 | — | EC50 | = | 29.5 | nM | 7.53 |
| CHEMBL1911151 | — | EC50 | = | 29.7 | nM | 7.53 |
| CHEMBL1911282 | — | EC50 | = | 33.8 | nM | 7.47 |
| CHEMBL1911272 | — | EC50 | = | 33.8 | nM | 7.47 |
| CHEMBL1911275 | — | EC50 | = | 64.9 | nM | 7.19 |
| CHEMBL1911157 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL1911283 | — | EC50 | = | 74.9 | nM | 7.13 |
| CHEMBL1911153 | — | EC50 | = | 108.0 | nM | 6.97 |
| CHEMBL1911269 | — | EC50 | = | 157.0 | nM | 6.80 |
| CHEMBL1911268 | — | EC50 | = | 216.0 | nM | 6.67 |
| CHEMBL1911148 | — | EC50 | = | 355.0 | nM | 6.45 |
| CHEMBL1911159 | — | EC50 | = | 1086.0 | nM | 5.96 |
| CHEMBL1911146 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL1911145 | — | EC50 | > | 5000.0 | nM | - |