Assay Detail
Binding
CHEMBL3860369
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R mutant phosphorylation in human patient derived H3255 cells incubated for 3 hrs by ELISA method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | H3255 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.49 | 8.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3939913 | — | — | 1 | 8.58 |
| CHEMBL3960167 | — | — | 1 | 8.52 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.39 |
| CHEMBL3787344 | NAZARTINIB | 2.0 | 1 | 8.21 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 7.86 |
| CHEMBL3972316 | — | — | 1 | 7.83 |
| CHEMBL3951434 | — | — | 1 | 7.34 |
| CHEMBL3901943 | — | — | 1 | 7.13 |
| CHEMBL3953921 | — | — | 1 | 6.38 |
| CHEMBL3961202 | — | — | 1 | 6.18 |
| CHEMBL3959632 | — | — | 1 | 5.98 |
| CHEMBL3966111 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3939913 | — | IC50 | = | 2.65 | nM | 8.58 |
| CHEMBL3960167 | — | IC50 | = | 3.05 | nM | 8.52 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3787344 | NAZARTINIB | IC50 | = | 6.11 | nM | 8.21 |
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL3972316 | — | IC50 | = | 14.84 | nM | 7.83 |
| CHEMBL3951434 | — | IC50 | = | 45.9 | nM | 7.34 |
| CHEMBL3901943 | — | IC50 | = | 74.9 | nM | 7.13 |
| CHEMBL3953921 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL3961202 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL3959632 | — | IC50 | = | 1041.0 | nM | 5.98 |
| CHEMBL3966111 | — | IC50 | > | 10000.0 | nM | - |