Assay Detail
Binding
CHEMBL5120450
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Inhibition of wild type EGFR expressed in human A-431 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-431 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.29 | 7.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.04 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.49 |
| CHEMBL5177023 | — | — | 1 | 6.24 |
| CHEMBL4443062 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 322.0 | nM | 6.49 |
| CHEMBL5177023 | — | IC50 | = | 577.0 | nM | 6.24 |
| CHEMBL4443062 | — | IC50 | = | 4213.0 | nM | 5.38 |