Assay Detail
Functional
CHEMBL5162341
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Antiproliferative activity against human SK-BR-3 cells overexpressing wild type HER2 assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-BR-3 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of SPH5030, a Selective, Potent, and Irreversible Tyrosine Kinase Inhibitor for HER2-Amplified and HER2-Mutant Cancer Treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.85 | 7.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.99 |
| CHEMBL3647420 | PYROTINIB | 3.0 | 1 | 7.85 |
| CHEMBL5178703 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | IC50 | = | 10.34 | nM | 7.99 |
| CHEMBL3647420 | PYROTINIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5178703 | — | IC50 | = | 20.09 | nM | 7.70 |