Assay Detail
Binding
CHEMBL4358574
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in human basophils assessed as reduction in anti-IgE mouse IgG1 antibody Le2-stimulated CD63 expression on basophil preincubated for 30 mins in presence of IgE antibody B11 followed by anti-IgE mouse IgG1 antibody Le2 stimulation and measured after 15 mins by flow cytometry
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.62 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297674 | BRANEBRUTINIB | 2.0 | 1 | 7.40 |
| CHEMBL4483575 | REMIBRUTINIB | 3.0 | 1 | 7.17 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 6.64 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 6.44 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 6.13 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297674 | BRANEBRUTINIB | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4483575 | REMIBRUTINIB | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4071161 | TIRABRUTINIB | IC50 | = | 363.0 | nM | 6.44 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 747.0 | nM | 6.13 |
| CHEMBL4072833 | EVOBRUTINIB | IC50 | = | 1182.0 | nM | 5.93 |