Assay Detail
Functional
CHEMBL5046859
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Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of highly potent and selective EGFR<sup>T790M/L858R</sup> TKIs against NSCLC based on molecular dynamic simulation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.75 | 6.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.47 |
| CHEMBL5093402 | — | — | 1 | 5.86 |
| CHEMBL5089161 | — | — | 1 | 5.58 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.57 |
| CHEMBL5083034 | — | — | 1 | 5.29 |
| CHEMBL5082074 | — | — | 1 | - |
| CHEMBL5087139 | — | — | 1 | - |
| CHEMBL5072451 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL5093402 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL5089161 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL939 | GEFITINIB | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL5083034 | — | IC50 | = | 5190.0 | nM | 5.29 |
| CHEMBL5082074 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5087139 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5072451 | — | IC50 | > | 100000.0 | nM | - |