Assay Detail
Functional
CHEMBL5255151
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Antiproliferative activity against mouse BAF3 cells harboring HER2-A775-G776 ins YVMA mutant after 72 hrs by celltiter-Glo luminescence assay
4
Total Activities
4
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
Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.86 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | 9.37 |
| CHEMBL5282641 | — | — | 1 | 9.05 |
| CHEMBL5288888 | — | — | 1 | 9.02 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545154 | POZIOTINIB | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL5282641 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL5288888 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 9.9 | nM | 8.00 |