Assay Detail
Binding
CHEMBL4670936
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His6-tagged HER2-A775_G776insYVMA mutant (703 to 1029 residues) (unknown origin) expressed in Sf9 insect cells using TK as substrate measured up to 2 to 40 mins by fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.65 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 9.12 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 8.20 |
| CHEMBL4757145 | — | — | 1 | 7.31 |
| CHEMBL4787483 | — | — | 1 | 7.27 |
| CHEMBL4756368 | — | — | 1 | 7.17 |
| CHEMBL4795165 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL180022 | NERATINIB | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4757145 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4787483 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL4756368 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL4795165 | — | Ki | = | 143.0 | nM | 6.84 |