Assay Detail
Binding
CHEMBL5251900
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR (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 | 6.72 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3973435 | — | — | 1 | 8.92 |
| CHEMBL3902845 | — | — | 1 | 8.77 |
| CHEMBL3936761 | ZANUBRUTINIB | 4.0 | 1 | 8.59 |
| CHEMBL3927293 | — | — | 1 | 7.96 |
| CHEMBL3935034 | — | — | 1 | 7.75 |
| CHEMBL5282956 | — | — | 1 | 7.75 |
| CHEMBL5266823 | — | — | 1 | 7.64 |
| CHEMBL5274187 | — | — | 1 | 7.21 |
| CHEMBL5272404 | — | — | 1 | 7.19 |
| CHEMBL5273525 | — | — | 1 | 7.00 |
| CHEMBL5268388 | — | — | 1 | 6.89 |
| CHEMBL5288582 | — | — | 1 | 6.57 |
| CHEMBL5288751 | — | — | 1 | 6.35 |
| CHEMBL5283553 | — | — | 1 | 6.22 |
| CHEMBL5276374 | — | — | 1 | 6.21 |
| CHEMBL5272121 | — | — | 1 | 6.18 |
| CHEMBL5266477 | — | — | 1 | 6.15 |
| CHEMBL5275348 | — | — | 1 | 5.96 |
| CHEMBL5289250 | — | — | 1 | 5.75 |
| CHEMBL5286702 | — | — | 1 | 5.70 |
| CHEMBL5265797 | — | — | 1 | 5.61 |
| CHEMBL3932338 | — | — | 1 | 5.58 |
| CHEMBL5266481 | — | — | 1 | 5.48 |
| CHEMBL5272694 | — | — | 1 | 5.35 |
| CHEMBL5266785 | — | — | 1 | 5.33 |
| CHEMBL5267491 | — | — | 1 | - |
| CHEMBL5278071 | — | — | 1 | - |
| CHEMBL5271932 | — | — | 1 | - |
| CHEMBL5269683 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3973435 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3902845 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3936761 | ZANUBRUTINIB | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3927293 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3935034 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5282956 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5266823 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5274187 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5272404 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL5273525 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5268388 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL5288582 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL5288751 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5283553 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL5276374 | — | IC50 | = | 621.0 | nM | 6.21 |
| CHEMBL5272121 | — | IC50 | = | 656.0 | nM | 6.18 |
| CHEMBL5266477 | — | IC50 | = | 713.0 | nM | 6.15 |
| CHEMBL5275348 | — | IC50 | = | 1092.0 | nM | 5.96 |
| CHEMBL5289250 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL5286702 | — | IC50 | = | 1999.0 | nM | 5.70 |
| CHEMBL5265797 | — | IC50 | = | 2458.0 | nM | 5.61 |
| CHEMBL3932338 | — | IC50 | = | 2613.0 | nM | 5.58 |
| CHEMBL5266481 | — | IC50 | = | 3326.0 | nM | 5.48 |
| CHEMBL5272694 | — | IC50 | = | 4496.0 | nM | 5.35 |
| CHEMBL5266785 | — | IC50 | = | 4713.0 | nM | 5.33 |
| CHEMBL5267491 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5278071 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5271932 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5269683 | — | IC50 | > | 1000.0 | nM | - |