Assay Detail
Binding
CHEMBL676069
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of heregulin-stimulated autophosphorylation of erbB2 in MDA-MB 453 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.02 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL136058 | — | — | 1 | 8.30 |
| CHEMBL342828 | — | — | 1 | 8.09 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | 3.0 | 1 | 8.05 |
| CHEMBL138940 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL136058 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL342828 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL138940 | — | IC50 | = | 24.0 | nM | 7.62 |