Assay Detail
Functional
CHEMBL5663212
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Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with ERBB2 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 | Homo sapiens |
| Cell Type | HCC827 |
| 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 | 8.14 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 8.70 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL939 | GEFITINIB | IC50 | = | 26.0 | nM | 7.58 |