Assay Detail
Binding
CHEMBL5626893
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system incubated for 1 hrs in presence of ATP by ADP-Glo reagent based assay
6
Total Activities
6
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 |
Publication
Cell-active, irreversible covalent inhibitors that selectively target the catalytic lysine of EGFR by using fluorosulfate-based SuFEx chemistry.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.33 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.92 |
| CHEMBL5633067 | — | — | 1 | 7.46 |
| CHEMBL5631574 | — | — | 1 | 7.39 |
| CHEMBL5631951 | — | — | 1 | 7.10 |
| CHEMBL5633759 | — | — | 1 | 6.77 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5633067 | — | IC50 | = | 35.1 | nM | 7.46 |
| CHEMBL5631574 | — | IC50 | = | 40.8 | nM | 7.39 |
| CHEMBL5631951 | — | IC50 | = | 79.3 | nM | 7.10 |
| CHEMBL5633759 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | - | — | - |