Assay Detail
Binding
CHEMBL1914161
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay
39
Total Activities
39
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 | 39 | 7.46 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL474189 | — | — | 1 | 8.28 |
| CHEMBL1911156 | — | — | 1 | 8.21 |
| CHEMBL1800985 | — | — | 1 | 8.11 |
| CHEMBL1911279 | — | — | 1 | 7.93 |
| CHEMBL1911278 | — | — | 1 | 7.91 |
| CHEMBL1911270 | — | — | 1 | 7.91 |
| CHEMBL1911154 | — | — | 1 | 7.87 |
| CHEMBL1911151 | — | — | 1 | 7.82 |
| CHEMBL1911276 | — | — | 1 | 7.80 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.79 |
| CHEMBL1911273 | — | — | 1 | 7.76 |
| CHEMBL1911150 | — | — | 1 | 7.75 |
| CHEMBL4296682 | — | — | 1 | 7.75 |
| CHEMBL1911152 | — | — | 1 | 7.74 |
| CHEMBL1911280 | — | — | 1 | 7.60 |
| CHEMBL1911277 | — | — | 1 | 7.56 |
| CHEMBL1911149 | — | — | 1 | 7.55 |
| CHEMBL1911155 | — | — | 1 | 7.54 |
| CHEMBL1911272 | — | — | 1 | 7.48 |
| CHEMBL1911269 | — | — | 1 | 7.47 |
| CHEMBL1911281 | — | — | 1 | 7.42 |
| CHEMBL1801012 | — | — | 1 | 7.39 |
| CHEMBL1911158 | — | — | 1 | 7.38 |
| CHEMBL1911147 | — | — | 1 | 7.33 |
| CHEMBL1911157 | — | — | 1 | 7.33 |
| CHEMBL1911282 | — | — | 1 | 7.30 |
| CHEMBL1911284 | — | — | 1 | 7.24 |
| CHEMBL1911283 | — | — | 1 | 7.11 |
| CHEMBL1911153 | — | — | 1 | 7.04 |
| CHEMBL1911145 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL474189 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL1911156 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1800985 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL1911279 | — | EC50 | = | 11.7 | nM | 7.93 |
| CHEMBL1911278 | — | EC50 | = | 12.4 | nM | 7.91 |
| CHEMBL1911270 | — | EC50 | = | 12.2 | nM | 7.91 |
| CHEMBL1911154 | — | EC50 | = | 13.6 | nM | 7.87 |
| CHEMBL1911151 | — | EC50 | = | 15.1 | nM | 7.82 |
| CHEMBL1911276 | — | EC50 | = | 15.7 | nM | 7.80 |
| CHEMBL131 | PREDNISOLONE | EC50 | = | 16.1 | nM | 7.79 |
| CHEMBL1911273 | — | EC50 | = | 17.4 | nM | 7.76 |
| CHEMBL1911150 | — | EC50 | = | 17.7 | nM | 7.75 |
| CHEMBL4296682 | — | EC50 | = | 17.7 | nM | 7.75 |
| CHEMBL1911152 | — | EC50 | = | 18.1 | nM | 7.74 |
| CHEMBL1911280 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1911277 | — | EC50 | = | 27.5 | nM | 7.56 |
| CHEMBL1911149 | — | EC50 | = | 28.3 | nM | 7.55 |
| CHEMBL1911155 | — | EC50 | = | 28.6 | nM | 7.54 |
| CHEMBL1911272 | — | EC50 | = | 33.2 | nM | 7.48 |
| CHEMBL1911269 | — | EC50 | = | 34.1 | nM | 7.47 |
| CHEMBL1911281 | — | EC50 | = | 37.9 | nM | 7.42 |
| CHEMBL1801012 | — | EC50 | = | 40.9 | nM | 7.39 |
| CHEMBL1911158 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1911147 | — | EC50 | = | 46.8 | nM | 7.33 |
| CHEMBL1911157 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1911282 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1911284 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1911283 | — | EC50 | = | 77.9 | nM | 7.11 |
| CHEMBL1911153 | — | EC50 | = | 90.8 | nM | 7.04 |
| CHEMBL1911145 | — | EC50 | = | 122.0 | nM | 6.91 |
| CHEMBL1911275 | — | EC50 | = | 124.0 | nM | 6.91 |
| CHEMBL1911268 | — | EC50 | = | 167.0 | nM | 6.78 |
| CHEMBL1911285 | — | EC50 | = | 183.0 | nM | 6.74 |
| CHEMBL1911159 | — | EC50 | = | 544.0 | nM | 6.26 |
| CHEMBL1911146 | — | EC50 | = | 654.0 | nM | 6.18 |
| CHEMBL1911148 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911160 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911144 | — | EC50 | > | 1500.0 | nM | - |
| CHEMBL1911271 | — | EC50 | > | 10000.0 | nM | - |