Assay Detail
Binding
CHEMBL5251899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells using Biotin-AVLESEEELYSSARQ-NH2 as substrate preincubated for 1 hrs followed by substrate addition in presence of ATP at Km concentration and measured after 1 hrs by TR-FRET assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 | 39 | 8.34 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 9.52 |
| CHEMBL5282956 | — | — | 1 | 9.48 |
| CHEMBL5275348 | — | — | 1 | 9.24 |
| CHEMBL3973435 | — | — | 1 | 9.20 |
| CHEMBL5288751 | — | — | 1 | 9.15 |
| CHEMBL3902845 | — | — | 1 | 9.10 |
| CHEMBL5271932 | — | — | 1 | 9.01 |
| CHEMBL5272404 | — | — | 1 | 9.00 |
| CHEMBL3927293 | — | — | 1 | 8.96 |
| CHEMBL5276374 | — | — | 1 | 8.96 |
| CHEMBL5286702 | — | — | 1 | 8.96 |
| CHEMBL3935034 | — | — | 1 | 8.92 |
| CHEMBL3932338 | — | — | 1 | 8.92 |
| CHEMBL5278071 | — | — | 1 | 8.92 |
| CHEMBL5272121 | — | — | 1 | 8.92 |
| CHEMBL5267491 | — | — | 1 | 8.89 |
| CHEMBL5269683 | — | — | 1 | 8.82 |
| CHEMBL5272694 | — | — | 1 | 8.82 |
| CHEMBL5274187 | — | — | 1 | 8.77 |
| CHEMBL5266481 | — | — | 1 | 8.77 |
| CHEMBL5283553 | — | — | 1 | 8.70 |
| CHEMBL5266477 | — | — | 1 | 8.70 |
| CHEMBL5289250 | — | — | 1 | 8.64 |
| CHEMBL5266785 | — | — | 1 | 8.12 |
| CHEMBL5270042 | — | — | 1 | 8.08 |
| CHEMBL5269628 | — | — | 1 | 7.85 |
| CHEMBL5280412 | — | — | 1 | 7.82 |
| CHEMBL5286643 | — | — | 1 | 7.80 |
| CHEMBL5287777 | — | — | 1 | 7.77 |
| CHEMBL5271354 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3936761 | ZANUBRUTINIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5282956 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL5275348 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL3973435 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL5288751 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3902845 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5271932 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL5272404 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5286702 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5276374 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3927293 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3935034 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3932338 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5278071 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5272121 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5267491 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5269683 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5272694 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5266481 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5274187 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5283553 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5266477 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5289250 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5266785 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5270042 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5269628 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5280412 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5286643 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5287777 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5271354 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5265797 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5283304 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5289355 | — | IC50 | = | 94.3 | nM | 7.03 |
| CHEMBL5275596 | — | IC50 | = | 95.4 | nM | 7.02 |
| CHEMBL5266823 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5288582 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5273525 | — | IC50 | = | 333.0 | nM | 6.48 |
| CHEMBL5268388 | — | IC50 | = | 864.0 | nM | 6.06 |
| CHEMBL5282462 | — | IC50 | > | 100.0 | nM | - |