Assay Detail
Functional
CHEMBL1914176
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiinflammatory activity in human whole blood assessed as inhibition of TNF-alpha-induced IL-8 production after overnight incubation by ELISA
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 | 10 | 6.05 | 6.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 6.91 |
| CHEMBL1911279 | — | — | 1 | 6.42 |
| CHEMBL4296682 | — | — | 1 | 6.27 |
| CHEMBL1911280 | — | — | 1 | 5.89 |
| CHEMBL1911272 | — | — | 1 | 5.83 |
| CHEMBL1911282 | — | — | 1 | 5.54 |
| CHEMBL1911281 | — | — | 1 | 5.51 |
| CHEMBL1911277 | — | — | 1 | - |
| CHEMBL1911269 | — | — | 1 | - |
| CHEMBL1911157 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | EC50 | = | 124.0 | nM | 6.91 |
| CHEMBL1911279 | — | EC50 | = | 382.0 | nM | 6.42 |
| CHEMBL4296682 | — | EC50 | = | 532.0 | nM | 6.27 |
| CHEMBL1911280 | — | EC50 | = | 1295.0 | nM | 5.89 |
| CHEMBL1911272 | — | EC50 | = | 1469.0 | nM | 5.83 |
| CHEMBL1911282 | — | EC50 | = | 2851.0 | nM | 5.54 |
| CHEMBL1911281 | — | EC50 | = | 3068.0 | nM | 5.51 |
| CHEMBL1911277 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL1911269 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL1911157 | — | EC50 | > | 20000.0 | nM | - |