Assay Detail
Functional
CHEMBL5153055
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Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
7
Total Activities
7
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 | 7 | 7.36 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 8.08 |
| CHEMBL5206110 | — | — | 1 | 7.84 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.28 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.27 |
| CHEMBL5180914 | — | — | 1 | 7.22 |
| CHEMBL4537790 | — | — | 1 | 7.12 |
| CHEMBL5206697 | — | — | 1 | 6.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4650319 | MOBOCERTINIB | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5206110 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 53.1 | nM | 7.28 |
| CHEMBL939 | GEFITINIB | IC50 | = | 53.6 | nM | 7.27 |
| CHEMBL5180914 | — | IC50 | = | 60.5 | nM | 7.22 |
| CHEMBL4537790 | — | IC50 | = | 76.4 | nM | 7.12 |
| CHEMBL5206697 | — | IC50 | = | 205.6 | nM | 6.69 |