Assay Detail
Binding
CHEMBL5251901
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Inhibition of TEC (unknown origin) preincubated for 1 hrs followed by substrate addition and measured after 1 hrs in the presence of ATP at Km concentration by TR-FRET assay
29
Total Activities
29
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 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 | 29 | 7.36 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 8.77 |
| CHEMBL3973435 | — | — | 1 | 8.60 |
| CHEMBL3935034 | — | — | 1 | 8.54 |
| CHEMBL3932338 | — | — | 1 | 8.44 |
| CHEMBL3902845 | — | — | 1 | 8.29 |
| CHEMBL3927293 | — | — | 1 | 8.23 |
| CHEMBL5274187 | — | — | 1 | 7.96 |
| CHEMBL5282956 | — | — | 1 | 7.89 |
| CHEMBL5266823 | — | — | 1 | 7.66 |
| CHEMBL5272404 | — | — | 1 | 7.62 |
| CHEMBL5272694 | — | — | 1 | 7.30 |
| CHEMBL5271932 | — | — | 1 | 7.30 |
| CHEMBL5266785 | — | — | 1 | 7.23 |
| CHEMBL5288751 | — | — | 1 | 7.22 |
| CHEMBL5273525 | — | — | 1 | 7.20 |
| CHEMBL5268388 | — | — | 1 | 7.11 |
| CHEMBL5275348 | — | — | 1 | 7.01 |
| CHEMBL5276374 | — | — | 1 | 7.00 |
| CHEMBL5272121 | — | — | 1 | 6.97 |
| CHEMBL5269683 | — | — | 1 | 6.87 |
| CHEMBL5278071 | — | — | 1 | 6.84 |
| CHEMBL5267491 | — | — | 1 | 6.75 |
| CHEMBL5266477 | — | — | 1 | 6.72 |
| CHEMBL5266481 | — | — | 1 | 6.67 |
| CHEMBL5288582 | — | — | 1 | 6.62 |
| CHEMBL5283553 | — | — | 1 | 6.53 |
| CHEMBL5286702 | — | — | 1 | 6.45 |
| CHEMBL5289250 | — | — | 1 | 6.26 |
| CHEMBL5265797 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3936761 | ZANUBRUTINIB | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3973435 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3935034 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3932338 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3902845 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3927293 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL5274187 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5282956 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5266823 | — | IC50 | = | 22.1 | nM | 7.66 |
| CHEMBL5272404 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5272694 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5271932 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5266785 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5288751 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5273525 | — | IC50 | = | 63.3 | nM | 7.20 |
| CHEMBL5268388 | — | IC50 | = | 77.5 | nM | 7.11 |
| CHEMBL5275348 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5276374 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5272121 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL5269683 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL5278071 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL5267491 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5266477 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL5266481 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL5288582 | — | IC50 | = | 241.4 | nM | 6.62 |
| CHEMBL5283553 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL5286702 | — | IC50 | = | 359.0 | nM | 6.45 |
| CHEMBL5289250 | — | IC50 | = | 551.0 | nM | 6.26 |
| CHEMBL5265797 | — | IC50 | > | 1000.0 | nM | - |