Assay Detail
Functional
CHEMBL5546056
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells harboring HER2 YVMA mutant by CellTiter-Glo assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of Novel 5,6-Dihydro-4<i>H</i>-pyrido[2,3,4-<i>de</i>]quinazoline Irreversible Inhibitors Targeting Both Wild-Type and A775_G776insYVMA Mutated HER2 Kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.73 | 8.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5563672 | — | — | 1 | 8.83 |
| CHEMBL5572660 | — | — | 1 | 8.42 |
| CHEMBL5584189 | — | — | 1 | 8.25 |
| CHEMBL5594407 | — | — | 1 | 8.12 |
| CHEMBL5591496 | — | — | 1 | 8.09 |
| CHEMBL5575930 | — | — | 1 | 8.06 |
| CHEMBL5572514 | — | — | 1 | 8.01 |
| CHEMBL5565503 | — | — | 1 | 7.99 |
| CHEMBL5570443 | — | — | 1 | 7.97 |
| CHEMBL5562735 | — | — | 1 | 7.97 |
| CHEMBL5574206 | — | — | 1 | 7.96 |
| CHEMBL5566173 | — | — | 1 | 7.90 |
| CHEMBL5566736 | — | — | 1 | 7.89 |
| CHEMBL5591662 | — | — | 1 | 7.85 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.84 |
| CHEMBL5566473 | — | — | 1 | 7.83 |
| CHEMBL5593219 | — | — | 1 | 7.80 |
| CHEMBL5566277 | — | — | 1 | 7.77 |
| CHEMBL5591255 | — | — | 1 | 7.69 |
| CHEMBL5567125 | — | — | 1 | 7.69 |
| CHEMBL3647420 | PYROTINIB | 3.0 | 1 | 7.61 |
| CHEMBL5571691 | — | — | 1 | 7.61 |
| CHEMBL5567355 | — | — | 1 | 7.59 |
| CHEMBL5571416 | — | — | 1 | 7.58 |
| CHEMBL5591930 | — | — | 1 | 7.52 |
| CHEMBL5569696 | — | — | 1 | 7.50 |
| CHEMBL5568970 | — | — | 1 | 7.35 |
| CHEMBL5569663 | — | — | 1 | 7.33 |
| CHEMBL5575614 | — | — | 1 | 7.26 |
| CHEMBL5593471 | — | — | 1 | 7.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5563672 | — | IC50 | = | 1.49 | nM | 8.83 |
| CHEMBL5572660 | — | IC50 | = | 3.82 | nM | 8.42 |
| CHEMBL5584189 | — | IC50 | = | 5.66 | nM | 8.25 |
| CHEMBL5594407 | — | IC50 | = | 7.63 | nM | 8.12 |
| CHEMBL5591496 | — | IC50 | = | 8.14 | nM | 8.09 |
| CHEMBL5575930 | — | IC50 | = | 8.69 | nM | 8.06 |
| CHEMBL5572514 | — | IC50 | = | 9.69 | nM | 8.01 |
| CHEMBL5565503 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL5570443 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL5562735 | — | IC50 | = | 10.68 | nM | 7.97 |
| CHEMBL5574206 | — | IC50 | = | 11.03 | nM | 7.96 |
| CHEMBL5566173 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL5566736 | — | IC50 | = | 12.84 | nM | 7.89 |
| CHEMBL5591662 | — | IC50 | = | 14.06 | nM | 7.85 |
| CHEMBL180022 | NERATINIB | IC50 | = | 14.59 | nM | 7.84 |
| CHEMBL5566473 | — | IC50 | = | 14.95 | nM | 7.83 |
| CHEMBL5593219 | — | IC50 | = | 15.75 | nM | 7.80 |
| CHEMBL5566277 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL5591255 | — | IC50 | = | 20.29 | nM | 7.69 |
| CHEMBL5567125 | — | IC50 | = | 20.44 | nM | 7.69 |
| CHEMBL3647420 | PYROTINIB | IC50 | = | 24.67 | nM | 7.61 |
| CHEMBL5571691 | — | IC50 | = | 24.82 | nM | 7.61 |
| CHEMBL5567355 | — | IC50 | = | 25.39 | nM | 7.59 |
| CHEMBL5571416 | — | IC50 | = | 26.22 | nM | 7.58 |
| CHEMBL5591930 | — | IC50 | = | 30.39 | nM | 7.52 |
| CHEMBL5569696 | — | IC50 | = | 31.64 | nM | 7.50 |
| CHEMBL5568970 | — | IC50 | = | 44.68 | nM | 7.35 |
| CHEMBL5569663 | — | IC50 | = | 47.04 | nM | 7.33 |
| CHEMBL5575614 | — | IC50 | = | 55.46 | nM | 7.26 |
| CHEMBL5593471 | — | IC50 | = | 54.5 | nM | 7.26 |
| CHEMBL5569311 | — | IC50 | = | 57.44 | nM | 7.24 |
| CHEMBL5591805 | — | IC50 | = | 58.54 | nM | 7.23 |
| CHEMBL5572476 | — | IC50 | = | 62.72 | nM | 7.20 |
| CHEMBL5572504 | — | IC50 | = | 71.05 | nM | 7.15 |
| CHEMBL5594898 | — | IC50 | = | 76.91 | nM | 7.11 |
| CHEMBL554 | LAPATINIB | IC50 | > | 2000.0 | nM | - |