Assay Detail
Binding
CHEMBL1116651
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HER2 by HTRF assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.72 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201179 | LAPATINIB DITOSYLATE | 4.0 | 1 | 8.52 |
| CHEMBL1080506 | — | — | 1 | 8.40 |
| CHEMBL1087368 | — | — | 1 | 8.15 |
| CHEMBL1079742 | ERLOTINIB HYDROCHLORIDE | 4.0 | 1 | 5.82 |
| CHEMBL1081849 | — | — | 1 | - |
| CHEMBL1082012 | — | — | 1 | - |
| CHEMBL1080812 | — | — | 1 | - |
| CHEMBL1080990 | — | — | 1 | - |
| CHEMBL1080271 | — | — | 1 | - |
| CHEMBL1080272 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201179 | LAPATINIB DITOSYLATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1080506 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1087368 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1079742 | ERLOTINIB HYDROCHLORIDE | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL1081849 | — | IC50 | - | — | - | |
| CHEMBL1082012 | — | IC50 | - | — | - | |
| CHEMBL1080812 | — | IC50 | - | — | - | |
| CHEMBL1080990 | — | IC50 | - | — | - | |
| CHEMBL1080271 | — | IC50 | - | — | - | |
| CHEMBL1080272 | — | IC50 | - | — | - |