Assay Detail
Functional
CHEMBL5215208
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Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay
6
Total Activities
6
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
The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.91 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3397300 | — | — | 1 | 7.55 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 7.40 |
| CHEMBL4203266 | — | — | 1 | 7.13 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.64 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 6.49 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3397300 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 39.9 | nM | 7.40 |
| CHEMBL4203266 | — | IC50 | = | 74.4 | nM | 7.13 |
| CHEMBL509032 | TAE-684 | IC50 | = | 229.3 | nM | 6.64 |
| CHEMBL3545360 | ASP-3026 | IC50 | = | 323.9 | nM | 6.49 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 576.6 | nM | 6.24 |