Assay Detail
Binding
CHEMBL4410890
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as reduction in cell growth incubated for 72 hrs in presence of 1 ug/ml Cetuximab by celltiter-glo luminescent cell viability assay
5
Total Activities
5
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
Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.63 | 6.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4452106 | — | — | 1 | 6.08 |
| CHEMBL4558528 | — | — | 1 | 5.57 |
| CHEMBL4533337 | — | — | 1 | 5.43 |
| CHEMBL4530686 | — | — | 1 | 5.42 |
| CHEMBL4520903 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4452106 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4558528 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4533337 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4530686 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4520903 | — | IC50 | > | 10000.0 | nM | - |