Assay Detail
Binding
CHEMBL5155250
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of sapitinib-BODIPY tracer from C-terminal NanoLuc-fused full length wild type EGFR (unknown origin) transfected in HEK293T cells incubated for 2 hrs by NanoBRET assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| 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 | 7 | 5.74 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5188250 | — | — | 1 | 6.48 |
| CHEMBL4098072 | — | — | 1 | 6.48 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.77 |
| CHEMBL5188399 | — | — | 1 | 5.17 |
| CHEMBL4214567 | — | — | 1 | 4.82 |
| CHEMBL5199122 | — | — | 1 | - |
| CHEMBL5183286 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5188250 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4098072 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5188399 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4214567 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5199122 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL5183286 | — | IC50 | > | 40000.0 | nM | - |