Assay Detail
Binding
CHEMBL5512284
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild-type HER2 phosphorylation in human BT-474 cells incubated for 1 hr by In-cell Western assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BT-474 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Potent and Selective Covalent Inhibitors of HER2<sup>WT</sup> and HER2<sup>YVMA</sup>.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.47 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3989868 | TUCATINIB | 4.0 | 1 | 8.15 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.44 |
| CHEMBL5566478 | — | — | 1 | 7.39 |
| CHEMBL5555280 | — | — | 1 | 7.31 |
| CHEMBL5561933 | — | — | 1 | 7.28 |
| CHEMBL5561503 | — | — | 1 | 7.23 |
| CHEMBL5542404 | — | — | 1 | 7.20 |
| CHEMBL5549855 | — | — | 1 | 7.14 |
| CHEMBL5542514 | — | — | 1 | 7.08 |
| CHEMBL5564323 | — | — | 1 | 7.00 |
| CHEMBL5549766 | — | — | 1 | 7.00 |
| CHEMBL5557178 | — | — | 1 | 6.80 |
| CHEMBL5523557 | — | — | 1 | 6.74 |
| CHEMBL5557512 | — | — | 1 | 6.71 |
| CHEMBL5558817 | — | — | 1 | 6.67 |
| CHEMBL5559677 | — | — | 1 | 6.66 |
| CHEMBL5559188 | — | — | 1 | 6.57 |
| CHEMBL5559752 | — | — | 1 | 6.51 |
| CHEMBL5561446 | — | — | 1 | 6.25 |
| CHEMBL5567982 | — | — | 1 | 5.98 |
| CHEMBL5527996 | — | — | 1 | 5.97 |
| CHEMBL5518102 | — | — | 1 | 5.92 |
| CHEMBL5531961 | — | — | 1 | 5.81 |
| CHEMBL5556683 | — | — | 1 | 5.70 |
| CHEMBL5561464 | — | — | 1 | 5.69 |
| CHEMBL5523491 | — | — | 1 | 5.46 |
| CHEMBL5557440 | — | — | 1 | 5.41 |
| CHEMBL5563970 | — | — | 1 | 5.39 |
| CHEMBL5527899 | — | — | 1 | 5.37 |
| CHEMBL5542937 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3989868 | TUCATINIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5566478 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5555280 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5561933 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5561503 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5542404 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5549855 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5542514 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5564323 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5549766 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5557178 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5523557 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL5557512 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL5558817 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL5559677 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL5559188 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL5559752 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL5561446 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL5567982 | — | IC50 | = | 1046.0 | nM | 5.98 |
| CHEMBL5527996 | — | IC50 | = | 1082.0 | nM | 5.97 |
| CHEMBL5518102 | — | IC50 | = | 1197.0 | nM | 5.92 |
| CHEMBL5531961 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL5556683 | — | IC50 | = | 2016.0 | nM | 5.70 |
| CHEMBL5561464 | — | IC50 | = | 2061.0 | nM | 5.69 |
| CHEMBL5523491 | — | IC50 | = | 3440.0 | nM | 5.46 |
| CHEMBL5557440 | — | IC50 | = | 3889.0 | nM | 5.41 |
| CHEMBL5563970 | — | IC50 | = | 4045.0 | nM | 5.39 |
| CHEMBL5527899 | — | IC50 | = | 4271.0 | nM | 5.37 |
| CHEMBL5542937 | — | IC50 | = | 4375.0 | nM | 5.36 |
| CHEMBL5563679 | — | IC50 | = | 4645.0 | nM | 5.33 |
| CHEMBL5559135 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5557058 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5555041 | — | IC50 | > | 5000.0 | nM | - |