Assay Detail
Binding
CHEMBL4670927
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibiton of EGFR L858R/T790M mutant (unknown origin) expressed in human NCI-H1975 cells assessed as reduction in EGFR induced cell viability after 96 hrs by CellTiter-Glo assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H1975 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.07 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.66 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 6.15 |
| CHEMBL4787483 | — | — | 1 | 6.13 |
| CHEMBL4757145 | — | — | 1 | 6.09 |
| CHEMBL4795165 | — | — | 1 | 5.57 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 4.83 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | - |
| CHEMBL4756368 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 714.0 | nM | 6.15 |
| CHEMBL4787483 | — | IC50 | = | 739.0 | nM | 6.13 |
| CHEMBL4757145 | — | IC50 | = | 807.0 | nM | 6.09 |
| CHEMBL4795165 | — | IC50 | = | 2664.0 | nM | 5.57 |
| CHEMBL554 | LAPATINIB | IC50 | = | 14781.0 | nM | 4.83 |
| CHEMBL180022 | NERATINIB | IC50 | < | 14.0 | nM | - |
| CHEMBL4756368 | — | IC50 | - | — | - |