Assay Detail
Binding
CHEMBL4724282
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HER2 (unknown origin) in presence of substrate incubated for 30 mins by ADP-Glo assay
7
Total Activities
7
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
HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and In Vitro and In Vivo Evaluation of Novel Lapatinib Congeners as Selective and Potent HER2 Inhibitors with Favorable Metabolic Stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.81 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4763836 | — | — | 1 | 8.27 |
| CHEMBL4796265 | — | — | 1 | 8.21 |
| CHEMBL4793731 | — | — | 1 | 8.08 |
| CHEMBL4783947 | — | — | 1 | 7.98 |
| CHEMBL4782561 | — | — | 1 | 7.92 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.22 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 7.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4763836 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4796265 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4793731 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4783947 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL4782561 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL180022 | NERATINIB | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL554 | LAPATINIB | IC50 | = | 95.5 | nM | 7.02 |