Assay Detail
Binding
CHEMBL5251905
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK phosphorylation at Tyr 223 residue in human Ramos cell incubated for 3 hrs by HTRF-based analysis
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ramos |
| 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 | 30 | 7.68 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297674 | BRANEBRUTINIB | 2.0 | 1 | 8.92 |
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 8.74 |
| CHEMBL3973435 | — | — | 1 | 8.49 |
| CHEMBL4650323 | TOLEBRUTINIB | 3.0 | 1 | 8.21 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.20 |
| CHEMBL5275348 | — | — | 1 | 7.97 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 7.96 |
| CHEMBL5276374 | — | — | 1 | 7.86 |
| CHEMBL5288751 | — | — | 1 | 7.84 |
| CHEMBL3932338 | — | — | 1 | 7.82 |
| CHEMBL5271932 | — | — | 1 | 7.70 |
| CHEMBL4650321 | ORELABRUTINIB | 3.0 | 1 | 7.70 |
| CHEMBL5272404 | — | — | 1 | 7.69 |
| CHEMBL5278071 | — | — | 1 | 7.67 |
| CHEMBL5266823 | — | — | 1 | 7.66 |
| CHEMBL5282956 | — | — | 1 | 7.66 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 7.66 |
| CHEMBL5267491 | — | — | 1 | 7.55 |
| CHEMBL5272121 | — | — | 1 | 7.55 |
| CHEMBL5269683 | — | — | 1 | 7.54 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 7.54 |
| CHEMBL5266481 | — | — | 1 | 7.48 |
| CHEMBL5286702 | — | — | 1 | 7.47 |
| CHEMBL5272694 | — | — | 1 | 7.31 |
| CHEMBL5289250 | — | — | 1 | 7.27 |
| CHEMBL5273525 | — | — | 1 | 7.20 |
| CHEMBL5283553 | — | — | 1 | 7.13 |
| CHEMBL5268388 | — | — | 1 | 7.11 |
| CHEMBL5266477 | — | — | 1 | 6.87 |
| CHEMBL5288582 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297674 | BRANEBRUTINIB | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3936761 | ZANUBRUTINIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3973435 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4650323 | TOLEBRUTINIB | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL5275348 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5276374 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL5288751 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL3932338 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL5271932 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4650321 | ORELABRUTINIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5272404 | — | IC50 | = | 20.3 | nM | 7.69 |
| CHEMBL5278071 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL5266823 | — | IC50 | = | 22.1 | nM | 7.66 |
| CHEMBL5282956 | — | IC50 | = | 21.9 | nM | 7.66 |
| CHEMBL4072833 | EVOBRUTINIB | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5267491 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5272121 | — | IC50 | = | 28.2 | nM | 7.55 |
| CHEMBL5269683 | — | IC50 | = | 29.1 | nM | 7.54 |
| CHEMBL4071161 | TIRABRUTINIB | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5266481 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5286702 | — | IC50 | = | 33.5 | nM | 7.47 |
| CHEMBL5272694 | — | IC50 | = | 49.4 | nM | 7.31 |
| CHEMBL5289250 | — | IC50 | = | 54.2 | nM | 7.27 |
| CHEMBL5273525 | — | IC50 | = | 63.3 | nM | 7.20 |
| CHEMBL5283553 | — | IC50 | = | 74.8 | nM | 7.13 |
| CHEMBL5268388 | — | IC50 | = | 77.5 | nM | 7.11 |
| CHEMBL5266477 | — | IC50 | = | 136.2 | nM | 6.87 |
| CHEMBL5288582 | — | IC50 | = | 241.4 | nM | 6.62 |