Assay Detail
Functional
CHEMBL5153058
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Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
3
Total Activities
3
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 | 3 | 7.88 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4537790 | — | — | 1 | 8.06 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.00 |
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4537790 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL4650319 | MOBOCERTINIB | IC50 | = | 27.1 | nM | 7.57 |