Assay Detail
Functional
CHEMBL5663180
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Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_S752InsV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
2
Total Activities
2
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
PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.68 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 8.85 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL939 | GEFITINIB | IC50 | = | 306.0 | nM | 6.51 |