Assay Detail
Binding
CHEMBL5512286
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Inhibition of wild-type human EGFR phosphorylation expressed in mouse NIH3T3 cells incubated for 1 hr by ELISA
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 5.78 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.28 |
| CHEMBL5566478 | — | — | 1 | 6.13 |
| CHEMBL5564323 | — | — | 1 | 5.91 |
| CHEMBL5561503 | — | — | 1 | 5.86 |
| CHEMBL5561933 | — | — | 1 | 5.67 |
| CHEMBL5523557 | — | — | 1 | 5.58 |
| CHEMBL5558817 | — | — | 1 | 5.38 |
| CHEMBL5555280 | — | — | 1 | 5.34 |
| CHEMBL5542514 | — | — | 1 | 5.34 |
| CHEMBL5557178 | — | — | 1 | 5.33 |
| CHEMBL5559677 | — | — | 1 | - |
| CHEMBL5556683 | — | — | 1 | - |
| CHEMBL5557058 | — | — | 1 | - |
| CHEMBL5557440 | — | — | 1 | - |
| CHEMBL5561464 | — | — | 1 | - |
| CHEMBL5563970 | — | — | 1 | - |
| CHEMBL5563679 | — | — | 1 | - |
| CHEMBL5559135 | — | — | 1 | - |
| CHEMBL5527899 | — | — | 1 | - |
| CHEMBL5555041 | — | — | 1 | - |
| CHEMBL5567982 | — | — | 1 | - |
| CHEMBL5549855 | — | — | 1 | - |
| CHEMBL5559752 | — | — | 1 | - |
| CHEMBL5561446 | — | — | 1 | - |
| CHEMBL5527996 | — | — | 1 | - |
| CHEMBL5542937 | — | — | 1 | - |
| CHEMBL5531961 | — | — | 1 | - |
| CHEMBL5559188 | — | — | 1 | - |
| CHEMBL5523491 | — | — | 1 | - |
| CHEMBL5542404 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5566478 | — | IC50 | = | 738.0 | nM | 6.13 |
| CHEMBL5564323 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL5561503 | — | IC50 | = | 1396.0 | nM | 5.86 |
| CHEMBL5561933 | — | IC50 | = | 2146.0 | nM | 5.67 |
| CHEMBL5523557 | — | IC50 | = | 2645.0 | nM | 5.58 |
| CHEMBL5558817 | — | IC50 | = | 4167.0 | nM | 5.38 |
| CHEMBL5555280 | — | IC50 | = | 4584.0 | nM | 5.34 |
| CHEMBL5542514 | — | IC50 | = | 4588.0 | nM | 5.34 |
| CHEMBL5557178 | — | IC50 | = | 4645.0 | nM | 5.33 |
| CHEMBL5557058 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3989868 | TUCATINIB | IC50 | > | 5000.0 | nM | - |
| CHEMBL5557440 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5561464 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5563970 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5563679 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5559135 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5527899 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5555041 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5549766 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5557512 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5518102 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5556683 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5559677 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5567982 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5549855 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5559752 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5561446 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5527996 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5542937 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5531961 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5559188 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5523491 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5542404 | — | IC50 | > | 5000.0 | nM | - |