Assay Detail
Binding
CHEMBL1914169
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay
36
Total Activities
36
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
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 | 36 | 6.75 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.68 |
| CHEMBL1911150 | — | — | 1 | 7.57 |
| CHEMBL1911278 | — | — | 1 | 7.54 |
| CHEMBL1911156 | — | — | 1 | 7.51 |
| CHEMBL1911279 | — | — | 1 | 7.46 |
| CHEMBL1911151 | — | — | 1 | 7.44 |
| CHEMBL1911273 | — | — | 1 | 7.43 |
| CHEMBL1911270 | — | — | 1 | 7.37 |
| CHEMBL1911152 | — | — | 1 | 7.11 |
| CHEMBL1911281 | — | — | 1 | 7.00 |
| CHEMBL1911149 | — | — | 1 | 6.98 |
| CHEMBL4296682 | — | — | 1 | 6.95 |
| CHEMBL1911282 | — | — | 1 | 6.89 |
| CHEMBL1911158 | — | — | 1 | 6.87 |
| CHEMBL1911272 | — | — | 1 | 6.85 |
| CHEMBL1911284 | — | — | 1 | 6.79 |
| CHEMBL1911157 | — | — | 1 | 6.79 |
| CHEMBL1911276 | — | — | 1 | 6.78 |
| CHEMBL1911144 | — | — | 1 | 6.73 |
| CHEMBL1911155 | — | — | 1 | 6.71 |
| CHEMBL1911160 | — | — | 1 | 6.70 |
| CHEMBL1911153 | — | — | 1 | 6.70 |
| CHEMBL1911277 | — | — | 1 | 6.69 |
| CHEMBL1911280 | — | — | 1 | 6.69 |
| CHEMBL1911154 | — | — | 1 | 6.62 |
| CHEMBL1911147 | — | — | 1 | 6.58 |
| CHEMBL1911269 | — | — | 1 | 6.39 |
| CHEMBL1911285 | — | — | 1 | 6.23 |
| CHEMBL1911283 | — | — | 1 | 6.21 |
| CHEMBL1911275 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1911150 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1911278 | — | EC50 | = | 28.6 | nM | 7.54 |
| CHEMBL1911156 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1911279 | — | EC50 | = | 34.4 | nM | 7.46 |
| CHEMBL1911151 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1911273 | — | EC50 | = | 36.7 | nM | 7.43 |
| CHEMBL1911270 | — | EC50 | = | 42.7 | nM | 7.37 |
| CHEMBL1911152 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL1911281 | — | EC50 | = | 99.3 | nM | 7.00 |
| CHEMBL1911149 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4296682 | — | EC50 | = | 113.4 | nM | 6.95 |
| CHEMBL1911282 | — | EC50 | = | 129.7 | nM | 6.89 |
| CHEMBL1911158 | — | EC50 | = | 134.0 | nM | 6.87 |
| CHEMBL1911272 | — | EC50 | = | 142.7 | nM | 6.85 |
| CHEMBL1911284 | — | EC50 | = | 162.0 | nM | 6.79 |
| CHEMBL1911157 | — | EC50 | = | 162.0 | nM | 6.79 |
| CHEMBL1911276 | — | EC50 | = | 167.1 | nM | 6.78 |
| CHEMBL1911144 | — | EC50 | = | 187.0 | nM | 6.73 |
| CHEMBL1911155 | — | EC50 | = | 196.0 | nM | 6.71 |
| CHEMBL1911160 | — | EC50 | = | 201.5 | nM | 6.70 |
| CHEMBL1911153 | — | EC50 | = | 201.0 | nM | 6.70 |
| CHEMBL1911277 | — | EC50 | = | 203.6 | nM | 6.69 |
| CHEMBL1911280 | — | EC50 | = | 205.0 | nM | 6.69 |
| CHEMBL1911154 | — | EC50 | = | 242.0 | nM | 6.62 |
| CHEMBL1911147 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1911269 | — | EC50 | = | 408.0 | nM | 6.39 |
| CHEMBL1911285 | — | EC50 | = | 592.0 | nM | 6.23 |
| CHEMBL1911283 | — | EC50 | = | 610.0 | nM | 6.21 |
| CHEMBL1911275 | — | EC50 | = | 721.1 | nM | 6.14 |
| CHEMBL1911268 | — | EC50 | = | 806.0 | nM | 6.09 |
| CHEMBL1911146 | — | EC50 | = | 1559.0 | nM | 5.81 |
| CHEMBL1911145 | — | EC50 | = | 1556.0 | nM | 5.81 |
| CHEMBL1911271 | — | EC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL1911148 | — | EC50 | = | 4360.0 | nM | 5.36 |
| CHEMBL1911159 | — | EC50 | > | 5000.0 | nM | - |