Assay Detail
Functional
CHEMBL5046857
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H1975 |
| 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 | 7.79 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5093402 | — | — | 1 | 8.70 |
| CHEMBL5072451 | — | — | 1 | 8.59 |
| CHEMBL5089161 | — | — | 1 | 8.40 |
| CHEMBL5083034 | — | — | 1 | 8.08 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.83 |
| CHEMBL5082074 | — | — | 1 | 7.53 |
| CHEMBL5087139 | — | — | 1 | 7.42 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5093402 | — | IC50 | = | 2.01 | nM | 8.70 |
| CHEMBL5072451 | — | IC50 | = | 2.58 | nM | 8.59 |
| CHEMBL5089161 | — | IC50 | = | 4.02 | nM | 8.40 |
| CHEMBL5083034 | — | IC50 | = | 8.31 | nM | 8.08 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL5082074 | — | IC50 | = | 29.7 | nM | 7.53 |
| CHEMBL5087139 | — | IC50 | = | 37.9 | nM | 7.42 |
| CHEMBL939 | GEFITINIB | IC50 | = | 1710.0 | nM | 5.77 |