Assay Detail
Binding
CHEMBL5155237
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human EGFR L858R mutant expressed in Sf9 insect cells in presence of ATP measured by HTRF 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 | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.47 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098072 | — | — | 1 | 9.59 |
| CHEMBL5183286 | — | — | 1 | 8.92 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.82 |
| CHEMBL5188399 | — | — | 1 | 8.70 |
| CHEMBL5188250 | — | — | 1 | 8.26 |
| CHEMBL5199122 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098072 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5183286 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5188399 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5188250 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5199122 | — | IC50 | = | 280.0 | nM | 6.55 |