Assay Detail
Binding
CHEMBL5140666
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by mobility shift assay
15
Total Activities
15
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
Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.61 | 6.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5173534 | — | — | 1 | 6.86 |
| CHEMBL5206298 | — | — | 1 | 6.79 |
| CHEMBL5201846 | — | — | 1 | 6.62 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.39 |
| CHEMBL5209075 | — | — | 1 | 6.38 |
| CHEMBL5174232 | — | — | 1 | - |
| CHEMBL5180848 | — | — | 1 | - |
| CHEMBL5191292 | — | — | 1 | - |
| CHEMBL5203821 | — | — | 1 | - |
| CHEMBL5175316 | — | — | 1 | - |
| CHEMBL5188618 | — | — | 1 | - |
| CHEMBL5199169 | — | — | 1 | - |
| CHEMBL5196254 | — | — | 1 | - |
| CHEMBL5189183 | — | — | 1 | - |
| CHEMBL5185772 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5173534 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5206298 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL5201846 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5209075 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL5174232 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5180848 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5191292 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5203821 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5175316 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5188618 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5199169 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5196254 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5189183 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5185772 | — | IC50 | > | 500.0 | nM | - |