Assay Detail
Functional
CHEMBL5153060
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Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
9
Total Activities
9
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 | 9 | 7.54 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.37 |
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 8.30 |
| CHEMBL4537790 | — | — | 1 | 8.19 |
| CHEMBL5206110 | — | — | 1 | 8.12 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.97 |
| CHEMBL5180914 | — | — | 1 | 7.75 |
| CHEMBL5206697 | — | — | 1 | 6.92 |
| CHEMBL5182465 | — | — | 1 | 6.70 |
| CHEMBL5190513 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4650319 | MOBOCERTINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4537790 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5206110 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL939 | GEFITINIB | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL5180914 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL5206697 | — | IC50 | = | 120.9 | nM | 6.92 |
| CHEMBL5182465 | — | IC50 | = | 197.5 | nM | 6.70 |
| CHEMBL5190513 | — | IC50 | = | 3101.2 | nM | 5.51 |