Assay Detail
Binding
CHEMBL1914165
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Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs 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 | 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 | 39 | 6.74 | 7.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1911273 | — | — | 1 | 7.49 |
| CHEMBL1911278 | — | — | 1 | 7.41 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.13 |
| CHEMBL1911156 | — | — | 1 | 7.12 |
| CHEMBL1911279 | — | — | 1 | 7.10 |
| CHEMBL1800985 | — | — | 1 | 7.07 |
| CHEMBL1911270 | — | — | 1 | 7.05 |
| CHEMBL4296682 | — | — | 1 | 7.01 |
| CHEMBL1911150 | — | — | 1 | 6.97 |
| CHEMBL474189 | — | — | 1 | 6.93 |
| CHEMBL1911151 | — | — | 1 | 6.90 |
| CHEMBL1911152 | — | — | 1 | 6.87 |
| CHEMBL1911282 | — | — | 1 | 6.78 |
| CHEMBL1911280 | — | — | 1 | 6.75 |
| CHEMBL1911281 | — | — | 1 | 6.72 |
| CHEMBL1911155 | — | — | 1 | 6.69 |
| CHEMBL1911272 | — | — | 1 | 6.62 |
| CHEMBL1911276 | — | — | 1 | 6.56 |
| CHEMBL1801012 | — | — | 1 | 6.43 |
| CHEMBL1911284 | — | — | 1 | 6.42 |
| CHEMBL1911157 | — | — | 1 | 6.30 |
| CHEMBL1911285 | — | — | 1 | 6.22 |
| CHEMBL1911275 | — | — | 1 | 6.15 |
| CHEMBL1911154 | — | — | 1 | 6.03 |
| CHEMBL1911147 | — | — | 1 | 5.66 |
| CHEMBL1911148 | — | — | 1 | - |
| CHEMBL1911158 | — | — | 1 | - |
| CHEMBL1911283 | — | — | 1 | - |
| CHEMBL1911277 | — | — | 1 | - |
| CHEMBL1911144 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1911273 | — | EC50 | = | 32.4 | nM | 7.49 |
| CHEMBL1911278 | — | EC50 | = | 39.2 | nM | 7.41 |
| CHEMBL131 | PREDNISOLONE | EC50 | = | 73.9 | nM | 7.13 |
| CHEMBL1911156 | — | EC50 | = | 75.4 | nM | 7.12 |
| CHEMBL1911279 | — | EC50 | = | 78.9 | nM | 7.10 |
| CHEMBL1800985 | — | EC50 | = | 85.7 | nM | 7.07 |
| CHEMBL1911270 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4296682 | — | EC50 | = | 98.5 | nM | 7.01 |
| CHEMBL1911150 | — | EC50 | = | 108.0 | nM | 6.97 |
| CHEMBL474189 | — | EC50 | = | 117.0 | nM | 6.93 |
| CHEMBL1911151 | — | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL1911152 | — | EC50 | = | 135.0 | nM | 6.87 |
| CHEMBL1911282 | — | EC50 | = | 165.0 | nM | 6.78 |
| CHEMBL1911280 | — | EC50 | = | 177.0 | nM | 6.75 |
| CHEMBL1911281 | — | EC50 | = | 192.0 | nM | 6.72 |
| CHEMBL1911155 | — | EC50 | = | 206.0 | nM | 6.69 |
| CHEMBL1911272 | — | EC50 | = | 242.0 | nM | 6.62 |
| CHEMBL1911276 | — | EC50 | = | 273.0 | nM | 6.56 |
| CHEMBL1801012 | — | EC50 | = | 372.0 | nM | 6.43 |
| CHEMBL1911284 | — | EC50 | = | 382.0 | nM | 6.42 |
| CHEMBL1911157 | — | EC50 | = | 496.0 | nM | 6.30 |
| CHEMBL1911285 | — | EC50 | = | 596.0 | nM | 6.22 |
| CHEMBL1911275 | — | EC50 | = | 702.0 | nM | 6.15 |
| CHEMBL1911154 | — | EC50 | = | 926.0 | nM | 6.03 |
| CHEMBL1911147 | — | EC50 | = | 2214.0 | nM | 5.66 |
| CHEMBL1911160 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911153 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911268 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911269 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911271 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911149 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911159 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911146 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911145 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911144 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911277 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911283 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911158 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1911148 | — | EC50 | > | 10000.0 | nM | - |