Assay Detail
Binding
CHEMBL673949
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of heregulin-stimulated autophosphorylation of ERBB2 receptor kinase in MDA-MB-453 cells.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-453 |
| 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. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.18 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54091 | — | — | 1 | 8.96 |
| CHEMBL31815 | — | — | 1 | 8.66 |
| CHEMBL53555 | — | — | 1 | 8.52 |
| CHEMBL51659 | — | — | 1 | 8.41 |
| CHEMBL31373 | — | — | 1 | 8.37 |
| CHEMBL285063 | — | — | 1 | 8.24 |
| CHEMBL280757 | — | — | 1 | 8.14 |
| CHEMBL430571 | — | — | 1 | 8.12 |
| CHEMBL53203 | — | — | 1 | 8.07 |
| CHEMBL28418 | — | — | 1 | 7.92 |
| CHEMBL53665 | — | — | 1 | 7.58 |
| CHEMBL443523 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54091 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL31815 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL53555 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL51659 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL31373 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL285063 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL280757 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL430571 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL53203 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL28418 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL53665 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL443523 | — | IC50 | = | 73.0 | nM | 7.14 |