Assay Detail
ADMET
CHEMBL1914172
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Induction of glutamine synthase expression in human MG63 cells after overnight incubation by spectrophotometry
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | MG-63 |
| Confidence | 1 — Organism |
| 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 | 3 | 7.25 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.72 |
| CHEMBL1911272 | — | — | 1 | 7.36 |
| CHEMBL4296682 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1911272 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4296682 | — | EC50 | = | 207.0 | nM | 6.68 |