Assay Detail
Functional
CHEMBL5711660
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Cytotoxicity against mouse Ba/F3 EGFR-Del19/T790M cells assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | Ba/F3 EGFR-Del19/T790M |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.68 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.37 |
| CHEMBL3787344 | NAZARTINIB | 2.0 | 1 | 7.73 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.11 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 6.92 |
| CHEMBL3397300 | — | — | 1 | 6.86 |
| CHEMBL4203266 | — | — | 1 | 6.76 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 6.41 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.29 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 6.00 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 5.67 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3787344 | NAZARTINIB | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 78.2 | nM | 7.11 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 120.2 | nM | 6.92 |
| CHEMBL3397300 | — | IC50 | = | 138.6 | nM | 6.86 |
| CHEMBL4203266 | — | IC50 | = | 175.4 | nM | 6.76 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 393.8 | nM | 6.41 |
| CHEMBL509032 | TAE-684 | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 1007.0 | nM | 6.00 |
| CHEMBL3545360 | ASP-3026 | IC50 | = | 2165.0 | nM | 5.67 |
| CHEMBL939 | GEFITINIB | IC50 | = | 4845.0 | nM | 5.32 |