Assay Detail
Binding
CHEMBL5155236
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human EGFR L858R/T790M double 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 | 0 — Uncurated / Unknown |
| 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 | 8.53 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098072 | — | — | 1 | 9.57 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.46 |
| CHEMBL5188399 | — | — | 1 | 8.82 |
| CHEMBL5188250 | — | — | 1 | 7.50 |
| CHEMBL5183286 | — | — | 1 | 7.29 |
| CHEMBL5199122 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098072 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL5188399 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5188250 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5183286 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5199122 | — | IC50 | > | 1000.0 | nM | - |