Assay Detail
Binding
CHEMBL5512285
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human HER2 YVMA mutant phosphorylation expressed in mouse NIH3T3 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 | NIH3T3 |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 6.50 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5566478 | — | — | 1 | 7.54 |
| CHEMBL5564323 | — | — | 1 | 7.51 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.47 |
| CHEMBL5561933 | — | — | 1 | 7.43 |
| CHEMBL5555280 | — | — | 1 | 7.38 |
| CHEMBL5549766 | — | — | 1 | 7.36 |
| CHEMBL5549855 | — | — | 1 | 7.29 |
| CHEMBL5561503 | — | — | 1 | 7.28 |
| CHEMBL5542514 | — | — | 1 | 7.28 |
| CHEMBL5542404 | — | — | 1 | 7.21 |
| CHEMBL5557178 | — | — | 1 | 7.10 |
| CHEMBL5559677 | — | — | 1 | 6.95 |
| CHEMBL5557512 | — | — | 1 | 6.94 |
| CHEMBL5558817 | — | — | 1 | 6.91 |
| CHEMBL5559752 | — | — | 1 | 6.84 |
| CHEMBL5559188 | — | — | 1 | 6.75 |
| CHEMBL5523557 | — | — | 1 | 6.67 |
| CHEMBL5561446 | — | — | 1 | 6.54 |
| CHEMBL3989868 | TUCATINIB | 4.0 | 1 | 6.36 |
| CHEMBL5567982 | — | — | 1 | 6.20 |
| CHEMBL5527996 | — | — | 1 | 6.09 |
| CHEMBL5531961 | — | — | 1 | 6.07 |
| CHEMBL5556683 | — | — | 1 | 5.80 |
| CHEMBL5555041 | — | — | 1 | 5.68 |
| CHEMBL5518102 | — | — | 1 | 5.65 |
| CHEMBL5563970 | — | — | 1 | 5.43 |
| CHEMBL5559135 | — | — | 1 | 5.41 |
| CHEMBL5563679 | — | — | 1 | 5.39 |
| CHEMBL5523491 | — | — | 1 | 5.36 |
| CHEMBL5527899 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5566478 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5564323 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5561933 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5555280 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5549766 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5549855 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5561503 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5542514 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5542404 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5557178 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5559677 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5557512 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL5558817 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL5559752 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL5559188 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL5523557 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL5561446 | — | IC50 | = | 292.0 | nM | 6.54 |
| CHEMBL3989868 | TUCATINIB | IC50 | = | 438.0 | nM | 6.36 |
| CHEMBL5567982 | — | IC50 | = | 637.0 | nM | 6.20 |
| CHEMBL5527996 | — | IC50 | = | 818.0 | nM | 6.09 |
| CHEMBL5531961 | — | IC50 | = | 858.0 | nM | 6.07 |
| CHEMBL5556683 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL5555041 | — | IC50 | = | 2102.0 | nM | 5.68 |
| CHEMBL5518102 | — | IC50 | = | 2258.0 | nM | 5.65 |
| CHEMBL5563970 | — | IC50 | = | 3752.0 | nM | 5.43 |
| CHEMBL5559135 | — | IC50 | = | 3889.0 | nM | 5.41 |
| CHEMBL5563679 | — | IC50 | = | 4061.0 | nM | 5.39 |
| CHEMBL5523491 | — | IC50 | = | 4377.0 | nM | 5.36 |
| CHEMBL5527899 | — | IC50 | = | 4422.0 | nM | 5.35 |
| CHEMBL5561464 | — | IC50 | = | 4601.0 | nM | 5.34 |
| CHEMBL5542937 | — | IC50 | = | 4804.0 | nM | 5.32 |
| CHEMBL5557058 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5557440 | — | IC50 | > | 5000.0 | nM | - |