Assay Detail
Binding
CHEMBL5162348
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HER2 D769H mutant (unknown origin) incubated for 120 mins in presence of 33P-ATP by P81 ion exchange cellulose chromatography
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 | 8.59 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5178703 | — | — | 1 | 9.38 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 8.21 |
| CHEMBL3647420 | PYROTINIB | 3.0 | 1 | 8.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5178703 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL180022 | NERATINIB | IC50 | = | 6.09 | nM | 8.21 |
| CHEMBL3647420 | PYROTINIB | IC50 | = | 6.65 | nM | 8.18 |