Assay Detail
Binding
CHEMBL4023752
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in human whole blood derived-basophils assessed as suppression of IgE mediated-FcepsilonR ligation-stimulated CD63 expression
5
Total Activities
5
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 GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.75 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4065122 | FENEBRUTINIB | 3.0 | 1 | 7.51 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 6.77 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 6.53 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 6.50 |
| CHEMBL3952795 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4065122 | FENEBRUTINIB | IC50 | = | 30.7 | nM | 7.51 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 296.9 | nM | 6.53 |
| CHEMBL4071161 | TIRABRUTINIB | IC50 | = | 312.3 | nM | 6.50 |
| CHEMBL3952795 | — | IC50 | = | 374.3 | nM | 6.43 |