Assay Detail
Binding
CHEMBL1116650
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HER2 in human SKBR3 cells by HTRF assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-BR-3 |
| Confidence | 9 — Direct 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 | 6.00 | 6.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201179 | LAPATINIB DITOSYLATE | 4.0 | 1 | 6.91 |
| CHEMBL1080272 | — | — | 1 | 6.21 |
| CHEMBL1082012 | — | — | 1 | 6.07 |
| CHEMBL1080990 | — | — | 1 | 6.03 |
| CHEMBL1087368 | — | — | 1 | 6.02 |
| CHEMBL1079742 | ERLOTINIB HYDROCHLORIDE | 4.0 | 1 | 5.72 |
| CHEMBL1081849 | — | — | 1 | 5.65 |
| CHEMBL1080271 | — | — | 1 | 5.42 |
| CHEMBL1080506 | — | — | 1 | - |
| CHEMBL1080812 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201179 | LAPATINIB DITOSYLATE | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL1080272 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1082012 | — | IC50 | = | 843.0 | nM | 6.07 |
| CHEMBL1080990 | — | IC50 | = | 934.0 | nM | 6.03 |
| CHEMBL1087368 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL1079742 | ERLOTINIB HYDROCHLORIDE | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL1081849 | — | IC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL1080271 | — | IC50 | = | 3840.0 | nM | 5.42 |
| CHEMBL1080506 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1080812 | — | IC50 | > | 5000.0 | nM | - |