Assay Detail
Binding
CHEMBL5577208
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M (unknown origin)
18
Total Activities
18
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
Exploring the structural activity relationship of the Osimertinib: A covalent inhibitor of double mutant EGFR<sup>L858R/T790M</sup> tyrosine kinase for the treatment of Non-Small Cell Lung Cancer (NSCLC).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.67 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5595344 | — | — | 1 | 8.70 |
| CHEMBL5593561 | — | — | 1 | 8.37 |
| CHEMBL5595805 | — | — | 1 | 8.24 |
| CHEMBL5088907 | — | — | 1 | 8.21 |
| CHEMBL5094406 | — | — | 1 | 8.10 |
| CHEMBL5591709 | — | — | 1 | 8.09 |
| CHEMBL5070579 | — | — | 1 | 8.07 |
| CHEMBL5594919 | — | — | 1 | 7.90 |
| CHEMBL5089912 | — | — | 1 | 7.37 |
| CHEMBL5173534 | — | — | 1 | 6.86 |
| CHEMBL5206298 | — | — | 1 | 6.79 |
| CHEMBL5201846 | — | — | 1 | 6.62 |
| CHEMBL5209075 | — | — | 1 | 6.38 |
| CHEMBL5090133 | — | — | 1 | - |
| CHEMBL5180848 | — | — | 1 | - |
| CHEMBL5191292 | — | — | 1 | - |
| CHEMBL5188618 | — | — | 1 | - |
| CHEMBL5199169 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5595344 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5593561 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5595805 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL5088907 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5094406 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5591709 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5070579 | — | IC50 | = | 8.58 | nM | 8.07 |
| CHEMBL5594919 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL5089912 | — | IC50 | = | 42.3 | nM | 7.37 |
| CHEMBL5173534 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5206298 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL5201846 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL5209075 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL5090133 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5180848 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5191292 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5188618 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5199169 | — | IC50 | > | 500.0 | nM | - |