Assay Detail
Functional
CHEMBL5355220
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Antiinflammatory activity in human PBMC assessed as inhibition of anti-IgM induced CD69 expression incubated for 2 hrs followed by goat F(ab') 2 anti-human IgM addition measured after 18 hrs by flow cytometry analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of orally active 1,4,5,6,8-pentaazaacenaphthylens as novel, selective, and potent covalent BTK inhibitors for the treatment of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.37 | 7.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.65 |
| CHEMBL5404368 | — | — | 1 | 7.28 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL5404368 | — | IC50 | = | 53.1 | nM | 7.28 |
| CHEMBL4072833 | EVOBRUTINIB | IC50 | = | 66.3 | nM | 7.18 |