Assay Detail
Functional
CHEMBL5260460
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Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
15
Total Activities
15
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
Addressing the Osimertinib Resistance Mutation EGFR-L858R/C797S with Reversible Aminopyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.47 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5270693 | — | — | 1 | 8.15 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.80 |
| CHEMBL5284924 | — | — | 1 | 7.03 |
| CHEMBL5289859 | — | — | 1 | 6.96 |
| CHEMBL5280082 | — | — | 1 | 6.70 |
| CHEMBL5288276 | — | — | 1 | 6.66 |
| CHEMBL5285052 | — | — | 1 | 6.64 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 6.53 |
| CHEMBL5287229 | — | — | 1 | 6.45 |
| CHEMBL5275642 | — | — | 1 | 6.21 |
| CHEMBL5278657 | — | — | 1 | 5.72 |
| CHEMBL5285308 | — | — | 1 | 5.69 |
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 5.57 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.53 |
| CHEMBL5269375 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5270693 | — | EC50 | = | 7.1 | nM | 8.15 |
| CHEMBL553 | ERLOTINIB | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5284924 | — | EC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5289859 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5280082 | — | EC50 | = | 202.0 | nM | 6.70 |
| CHEMBL5288276 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5285052 | — | EC50 | = | 227.0 | nM | 6.64 |
| CHEMBL3545311 | BRIGATINIB | EC50 | = | 295.0 | nM | 6.53 |
| CHEMBL5287229 | — | EC50 | = | 354.0 | nM | 6.45 |
| CHEMBL5275642 | — | EC50 | = | 615.0 | nM | 6.21 |
| CHEMBL5278657 | — | EC50 | = | 1884.0 | nM | 5.72 |
| CHEMBL5285308 | — | EC50 | = | 2059.0 | nM | 5.69 |
| CHEMBL4650319 | MOBOCERTINIB | EC50 | = | 2711.0 | nM | 5.57 |
| CHEMBL3353410 | OSIMERTINIB | EC50 | = | 2956.0 | nM | 5.53 |
| CHEMBL5269375 | — | EC50 | = | 3754.0 | nM | 5.43 |