Assay Detail
Binding
CHEMBL4332364
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged HER2 catalytic domain (676 to 1255 residues) expressed in baculovirus expression system using TK-biotin peptide as substrate measured after 10 mins by HTRF assay
9
Total Activities
9
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
Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.06 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4591886 | — | — | 1 | 7.96 |
| CHEMBL4474073 | — | — | 1 | 7.41 |
| CHEMBL4473875 | — | — | 1 | 7.38 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.13 |
| CHEMBL4450824 | — | — | 1 | 7.08 |
| CHEMBL4592101 | — | — | 1 | 6.88 |
| CHEMBL4577883 | — | — | 1 | 6.83 |
| CHEMBL4447976 | — | — | 1 | 6.58 |
| CHEMBL4443188 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4591886 | — | IC50 | = | 10.94 | nM | 7.96 |
| CHEMBL4474073 | — | IC50 | = | 39.26 | nM | 7.41 |
| CHEMBL4473875 | — | IC50 | = | 42.11 | nM | 7.38 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 73.72 | nM | 7.13 |
| CHEMBL4450824 | — | IC50 | = | 83.84 | nM | 7.08 |
| CHEMBL4592101 | — | IC50 | = | 131.6 | nM | 6.88 |
| CHEMBL4577883 | — | IC50 | = | 148.3 | nM | 6.83 |
| CHEMBL4447976 | — | IC50 | = | 261.8 | nM | 6.58 |
| CHEMBL4443188 | — | IC50 | = | 482.1 | nM | 6.32 |