Assay Detail
Binding
CHEMBL5251929
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FLAG-tagged TEC autophosphorylation in HEK293 cells incubated for 2 hrs by MSD electrochemiluminescence immunoassay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.80 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297674 | BRANEBRUTINIB | 2.0 | 1 | 8.96 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.48 |
| CHEMBL3973435 | — | — | 1 | 8.17 |
| CHEMBL4650323 | TOLEBRUTINIB | 3.0 | 1 | 8.11 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 7.84 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 7.70 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 7.70 |
| CHEMBL4650321 | ORELABRUTINIB | 3.0 | 1 | 7.43 |
| CHEMBL5288751 | — | — | 1 | 6.98 |
| CHEMBL5276374 | — | — | 1 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297674 | BRANEBRUTINIB | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3973435 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4650323 | TOLEBRUTINIB | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4071161 | TIRABRUTINIB | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4072833 | EVOBRUTINIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4650321 | ORELABRUTINIB | IC50 | = | 37.2 | nM | 7.43 |
| CHEMBL5288751 | — | IC50 | = | 103.8 | nM | 6.98 |
| CHEMBL5276374 | — | IC50 | = | 223.1 | nM | 6.65 |