Assay Detail
Binding
CHEMBL1914151
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluorescently labeled ligand from progesterone receptor by fluorescence polarization assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 |
|---|---|---|---|
| Ki | 8 | 6.34 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1800985 | — | — | 1 | 7.28 |
| CHEMBL1801012 | — | — | 1 | 6.56 |
| CHEMBL1911151 | — | — | 1 | 6.54 |
| CHEMBL1911152 | — | — | 1 | 6.51 |
| CHEMBL1911270 | — | — | 1 | 5.91 |
| CHEMBL1911272 | — | — | 1 | 5.82 |
| CHEMBL4296682 | — | — | 1 | 5.74 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1800985 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL1801012 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL1911151 | — | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL1911152 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL1911270 | — | Ki | = | 1228.0 | nM | 5.91 |
| CHEMBL1911272 | — | Ki | = | 1529.0 | nM | 5.82 |
| CHEMBL4296682 | — | Ki | = | 1829.0 | nM | 5.74 |
| CHEMBL131 | PREDNISOLONE | Ki | > | 6000.0 | nM | - |