Assay Detail
Binding
CHEMBL3815440
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged human recombinant Her2 (676 to 1255 residues) expressed in baculovirus by fluorescence based assay
7
Total Activities
7
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
Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.54 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3814812 | — | — | 1 | 7.92 |
| CHEMBL3814021 | — | — | 1 | 7.72 |
| CHEMBL3633928 | — | — | 1 | 7.57 |
| CHEMBL3814846 | — | — | 1 | 7.49 |
| CHEMBL3813728 | — | — | 1 | 7.48 |
| CHEMBL3814940 | — | — | 1 | 7.39 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3814812 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL3814021 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL3633928 | — | IC50 | = | 26.8 | nM | 7.57 |
| CHEMBL3814846 | — | IC50 | = | 32.3 | nM | 7.49 |
| CHEMBL3813728 | — | IC50 | = | 33.1 | nM | 7.48 |
| CHEMBL3814940 | — | IC50 | = | 40.6 | nM | 7.39 |
| CHEMBL554 | LAPATINIB | IC50 | = | 60.1 | nM | 7.22 |