Assay Detail
Functional
CHEMBL5546058
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771insSVD by CellTiter-Glo assay
15
Total Activities
15
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 | 15 | 6.99 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.70 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.70 |
| CHEMBL5565503 | — | — | 1 | 7.21 |
| CHEMBL5572670 | — | — | 1 | 7.19 |
| CHEMBL5572504 | — | — | 1 | 7.18 |
| CHEMBL5562735 | — | — | 1 | 7.16 |
| CHEMBL5584189 | — | — | 1 | 7.10 |
| CHEMBL5574232 | — | — | 1 | 6.86 |
| CHEMBL5591805 | — | — | 1 | 6.79 |
| CHEMBL5569311 | — | — | 1 | 6.73 |
| CHEMBL5569244 | — | — | 1 | 6.71 |
| CHEMBL5575614 | — | — | 1 | 6.69 |
| CHEMBL5572476 | — | — | 1 | 6.68 |
| CHEMBL5593219 | — | — | 1 | 6.66 |
| CHEMBL5593471 | — | — | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | IC50 | = | 19.96 | nM | 7.70 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 19.96 | nM | 7.70 |
| CHEMBL5565503 | — | IC50 | = | 61.6 | nM | 7.21 |
| CHEMBL5572670 | — | IC50 | = | 64.95 | nM | 7.19 |
| CHEMBL5572504 | — | IC50 | = | 66.1 | nM | 7.18 |
| CHEMBL5562735 | — | IC50 | = | 69.76 | nM | 7.16 |
| CHEMBL5584189 | — | IC50 | = | 79.58 | nM | 7.10 |
| CHEMBL5574232 | — | IC50 | = | 137.8 | nM | 6.86 |
| CHEMBL5591805 | — | IC50 | = | 163.3 | nM | 6.79 |
| CHEMBL5569311 | — | IC50 | = | 187.9 | nM | 6.73 |
| CHEMBL5569244 | — | IC50 | = | 193.7 | nM | 6.71 |
| CHEMBL5575614 | — | IC50 | = | 202.5 | nM | 6.69 |
| CHEMBL5572476 | — | IC50 | = | 207.3 | nM | 6.68 |
| CHEMBL5593219 | — | IC50 | = | 217.7 | nM | 6.66 |
| CHEMBL5593471 | — | IC50 | = | 277.2 | nM | 6.56 |