Assay Detail
Binding
CHEMBL4670931
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-tagged EGFR (669 to 1210 residues) expressed in baculovirus infected Sf9 insect cells using TK as substrate preincubated for 30 mins followed by substrate addition and measured after 25 mins by HTRF assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| 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 |
|---|---|---|---|
| IC50 | 8 | 10.05 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 10.70 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 10.22 |
| CHEMBL4756368 | — | — | 1 | 10.15 |
| CHEMBL4787483 | — | — | 1 | 10.10 |
| CHEMBL4757145 | — | — | 1 | 10.05 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.70 |
| CHEMBL4795165 | — | — | 1 | 9.40 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL554 | LAPATINIB | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL4756368 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL4787483 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL4757145 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4795165 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 0.01 | nM | - |