Assay Detail
Functional
CHEMBL5046860
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Antiproliferative activity against human NCI-H1299 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 | NCI-H1299 |
| 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 | 5.47 | 5.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5093402 | — | — | 1 | 5.75 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.55 |
| CHEMBL5089161 | — | — | 1 | 5.40 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.39 |
| CHEMBL5083034 | — | — | 1 | 5.28 |
| CHEMBL5082074 | — | — | 1 | - |
| CHEMBL5087139 | — | — | 1 | - |
| CHEMBL5072451 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5093402 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 2840.0 | nM | 5.55 |
| CHEMBL5089161 | — | IC50 | = | 3980.0 | nM | 5.40 |
| CHEMBL939 | GEFITINIB | IC50 | = | 4050.0 | nM | 5.39 |
| CHEMBL5083034 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5082074 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5087139 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5072451 | — | IC50 | > | 100000.0 | nM | - |