Assay Detail
Binding
CHEMBL5162369
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HER2 (unknown origin)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 8.28 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3647420 | PYROTINIB | 3.0 | 1 | 8.35 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 8.34 |
| CHEMBL3989868 | TUCATINIB | 4.0 | 1 | 8.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3647420 | PYROTINIB | IC50 | = | 4.43 | nM | 8.35 |
| CHEMBL180022 | NERATINIB | IC50 | = | 4.57 | nM | 8.34 |
| CHEMBL3989868 | TUCATINIB | IC50 | = | 6.9 | nM | 8.16 |