Assay Detail
Functional
CHEMBL5153057
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.99 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5206110 | — | — | 1 | 8.21 |
| CHEMBL4537790 | — | — | 1 | 7.96 |
| CHEMBL5180914 | — | — | 1 | 7.75 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.27 |
| CHEMBL5206697 | — | — | 1 | 6.85 |
| CHEMBL5182465 | — | — | 1 | 6.12 |
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 5.95 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5206110 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4537790 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL5180914 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL939 | GEFITINIB | IC50 | = | 54.2 | nM | 7.27 |
| CHEMBL5206697 | — | IC50 | = | 141.4 | nM | 6.85 |
| CHEMBL5182465 | — | IC50 | = | 749.6 | nM | 6.12 |
| CHEMBL4650319 | MOBOCERTINIB | IC50 | = | 1133.7 | nM | 5.95 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 1475.0 | nM | 5.83 |