Assay Detail
Binding
CHEMBL5162302
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Inhibition of wild type human GST-tagged HER2 (676 to end residues) expressed in baculovirus infected Sf9 cells incubated for 30 mins in presence of ATP by HTRF analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 | 21 | 8.39 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5176920 | — | — | 1 | 8.97 |
| CHEMBL5193451 | — | — | 1 | 8.85 |
| CHEMBL5179954 | — | — | 1 | 8.85 |
| CHEMBL5184610 | — | — | 1 | 8.78 |
| CHEMBL5192750 | — | — | 1 | 8.77 |
| CHEMBL5175489 | — | — | 1 | 8.71 |
| CHEMBL5190132 | — | — | 1 | 8.62 |
| CHEMBL5203179 | — | — | 1 | 8.59 |
| CHEMBL5175873 | — | — | 1 | 8.54 |
| CHEMBL5176854 | — | — | 1 | 8.47 |
| CHEMBL5178703 | — | — | 1 | 8.46 |
| CHEMBL5181694 | — | — | 1 | 8.43 |
| CHEMBL5183924 | — | — | 1 | 8.39 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 8.25 |
| CHEMBL5180965 | — | — | 1 | 8.20 |
| CHEMBL5201973 | — | — | 1 | 8.19 |
| CHEMBL5170965 | — | — | 1 | 8.14 |
| CHEMBL3647420 | PYROTINIB | 3.0 | 1 | 8.04 |
| CHEMBL5209046 | — | — | 1 | 7.97 |
| CHEMBL5202846 | — | — | 1 | 7.80 |
| CHEMBL5180725 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5176920 | — | IC50 | = | 1.06 | nM | 8.97 |
| CHEMBL5193451 | — | IC50 | = | 1.43 | nM | 8.85 |
| CHEMBL5179954 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5184610 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL5192750 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5175489 | — | IC50 | = | 1.93 | nM | 8.71 |
| CHEMBL5190132 | — | IC50 | = | 2.41 | nM | 8.62 |
| CHEMBL5203179 | — | IC50 | = | 2.55 | nM | 8.59 |
| CHEMBL5175873 | — | IC50 | = | 2.85 | nM | 8.54 |
| CHEMBL5176854 | — | IC50 | = | 3.38 | nM | 8.47 |
| CHEMBL5178703 | — | IC50 | = | 3.51 | nM | 8.46 |
| CHEMBL5181694 | — | IC50 | = | 3.68 | nM | 8.43 |
| CHEMBL5183924 | — | IC50 | = | 4.05 | nM | 8.39 |
| CHEMBL180022 | NERATINIB | IC50 | = | 5.57 | nM | 8.25 |
| CHEMBL5180965 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL5201973 | — | IC50 | = | 6.42 | nM | 8.19 |
| CHEMBL5170965 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3647420 | PYROTINIB | IC50 | = | 9.07 | nM | 8.04 |
| CHEMBL5209046 | — | IC50 | = | 10.77 | nM | 7.97 |
| CHEMBL5202846 | — | IC50 | = | 16.01 | nM | 7.80 |
| CHEMBL5180725 | — | IC50 | = | 62.26 | nM | 7.21 |