Assay Detail
Functional
CHEMBL4626971
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Antiinflammatory activity in human PBMC assessed as reduction in LPS-induced IL-6 production incubated for 18 to 24 hrs by mesoscale assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.87 | 7.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4639128 | GSK778 | — | 1 | 7.20 |
| CHEMBL2017291 | — | — | 1 | 6.90 |
| CHEMBL4638144 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4639128 | GSK778 | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL2017291 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4638144 | — | IC50 | = | 316.23 | nM | 6.50 |